Category: 256935-86-1

On February 1, 2010, Mavunkel, Babu J.; Perumattam, John J.; Tan, Xuefei; Luedtke, Gregory R.; Lu, Qing; Lim, Don; Kizer, Darin; Dugar, Sundeep; Chakravarty, Sarvajit; Xu, Yong-jin; Jung, Joon; Liclican, Albert; Levy, Daniel E.; Tabora, Jocelyn published an article.HPLC of Formula: 256935-86-1 The title of the article was Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors. And the article contained the following:

The design and synthesis of a new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine heterocyclic oxalyl amides are described. Many of these compounds showed low-nanomolar activities in p38α enzymic and cell-based cytokine TNFα production inhibition assays. The optimal linkers between the piperidine and the oxalyl amide were found to be [6,5] fused ring heterocycles. Substituted indoles and azaindoles were favored structural motifs in the cellular assay. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).HPLC of Formula: 256935-86-1

The Article related to piperidine based heterocyclic oxalyl amide preparation antiinflammatory, p38alpha map kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On February 1, 2010, Mavunkel, Babu J.; Perumattam, John J.; Tan, Xuefei; Luedtke, Gregory R.; Lu, Qing; Lim, Don; Kizer, Darin; Dugar, Sundeep; Chakravarty, Sarvajit; Xu, Yong-jin; Jung, Joon; Liclican, Albert; Levy, Daniel E.; Tabora, Jocelyn published an article.HPLC of Formula: 256935-86-1 The title of the article was Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors. And the article contained the following:

The design and synthesis of a new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine heterocyclic oxalyl amides are described. Many of these compounds showed low-nanomolar activities in p38α enzymic and cell-based cytokine TNFα production inhibition assays. The optimal linkers between the piperidine and the oxalyl amide were found to be [6,5] fused ring heterocycles. Substituted indoles and azaindoles were favored structural motifs in the cellular assay. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).HPLC of Formula: 256935-86-1

The Article related to piperidine based heterocyclic oxalyl amide preparation antiinflammatory, p38alpha map kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Sekhar, Abinitha S.; Saranya, T. S.; Baskar, Vaishnav; Manakadan, Asha Ashokan published an article in 2016, the title of the article was In silico approach of apoptosis induing ability of different indole derivatives by interaction with caspase9.Related Products of 256935-86-1 And the article contains the following content:

Indole compounds are well known for their wide variety of pharmacol. activities. It is the combination of benzene with pyrrole ring. Compounds having indole group are biol. important. They are used as antimicrobial, antiviral, antitubercular, antiinflammatory, anticancer, ant-diabetic and anticonvulsant agents. Because of the wide variety of biol. application, several substituted indole derivatives are studied for their mol. structure, mol. docking and bioavailability. The purpose of the study is to carry out the docking studies of indole derivatives containing electrophilic substitution and nucleophilic substitution with the anticancer target casp9. Fifty compounds were designed and by using Argus lab version 4.0.1. Their docking score was calculated and compared with the standard drug casodex. The drug likeness of compounds was performed using Lipinski rule of five. Result showed that 1,1′-(1H-indole-5,6-diyl)diethanone and 5-(trichloromethyl)-1H-indole and the phytoconstituent curcumin showed better docking score than that of the standard drug casodex. It is concluded that certain indole derivatives show greater affinity with casp9 protein. These compounds may be helpful in studying anticancer targets for casp9 protein. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Related Products of 256935-86-1

The Article related to indole derivative induce apoptosis ability anticancer target caspase protein, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Related Products of 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On February 10, 2000, Gwaltney, Stephen L., II; Jae, Hwan-Soo; Kalvin, Douglas M.; Liu, Gang; Sham, Hing L.; Li, Qun; Claiborne, Akiyo K.; Wang, Le; Barr, Kenneth J.; Woods, Keith W. published a patent.Safety of 6-Chloro-1H-indole-5-carboxylic acid The title of the patent was Preparation of substituted oxazolines as antiproliferative agents. And the patent contained the following:

The title compounds [I; R1-R3 = alkyl, alkoxy, thioalkoxy; R4, R5 = H, alkyl; R6 = (un)substituted aryl, heterocyclyl, cycloalkyl, etc.], useful for treating cancer, were prepared E.g., a multi-step synthesis of I [R1-R3 = 3,4,5-(MeO)3; R4, R5 = H; R6 = 4-Me2NC6H4] which showed 100% inhibition in both 48-h cellular proliferation assays that used human colon adenocarcinoma, MDR pos. and human lung cell carcinoma, MDR neg., was given. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Safety of 6-Chloro-1H-indole-5-carboxylic acid

The Article related to oxazoline preparation antiproliferative antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Safety of 6-Chloro-1H-indole-5-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On May 8, 2001, Gwaltney, Stephen L., II; Jae, Hwan-Soo; Kalvin, Douglas M.; Liu, Gang; Sham, Hing L.; Li, Qun; Claiborne, Akiyo K.; Wang, Le; Barr, Kenneth J.; Woods, Keith W. published a patent.HPLC of Formula: 256935-86-1 The title of the patent was Preparation of oxazoline antiproliferative agents. And the patent contained the following:

R2ZR [I; R = alkyl-, alkoxy, or alkylthio-trisubstituted Ph; R2 = (un)substituted cycloalk(en)yl, -heterocyclyl, -aryl, etc.; Z = (4-alkyl)-2-oxazoline-2,5-diyl or 4,4-dialkyl-2-oxazoline-2,5-diyl] were prepared Thus, 3,4,5-trimethoxybenzaldehyde was condensed with MeNO2 and the reduced product amidated by 4-(Me2N)C6H4COCl to give, after cyclization, I [R = C6H2(OMe)3-3,4,5, R2 = C6H4(NMe2)-4, Z = 2-oxazoline-2,5-diyl]. Data for biol. activity of I were given. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).HPLC of Formula: 256935-86-1

The Article related to oxazoline preparation antiproliferative agent, antitumor agent oxazoline preparation, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.HPLC of Formula: 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On February 10, 2000, Gwaltney, Stephen L., II; Jae, Hwan-Soo; Kalvin, Douglas M.; Liu, Gang; Sham, Hing L.; Li, Qun; Claiborne, Akiyo K.; Wang, Le; Barr, Kenneth J.; Woods, Keith W. published a patent.Safety of 6-Chloro-1H-indole-5-carboxylic acid The title of the patent was Preparation of substituted oxazolines as antiproliferative agents. And the patent contained the following:

The title compounds [I; R1-R3 = alkyl, alkoxy, thioalkoxy; R4, R5 = H, alkyl; R6 = (un)substituted aryl, heterocyclyl, cycloalkyl, etc.], useful for treating cancer, were prepared E.g., a multi-step synthesis of I [R1-R3 = 3,4,5-(MeO)3; R4, R5 = H; R6 = 4-Me2NC6H4] which showed 100% inhibition in both 48-h cellular proliferation assays that used human colon adenocarcinoma, MDR pos. and human lung cell carcinoma, MDR neg., was given. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Safety of 6-Chloro-1H-indole-5-carboxylic acid

The Article related to oxazoline preparation antiproliferative antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Safety of 6-Chloro-1H-indole-5-carboxylic acid

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On May 8, 2001, Gwaltney, Stephen L., II; Jae, Hwan-Soo; Kalvin, Douglas M.; Liu, Gang; Sham, Hing L.; Li, Qun; Claiborne, Akiyo K.; Wang, Le; Barr, Kenneth J.; Woods, Keith W. published a patent.HPLC of Formula: 256935-86-1 The title of the patent was Preparation of oxazoline antiproliferative agents. And the patent contained the following:

R2ZR [I; R = alkyl-, alkoxy, or alkylthio-trisubstituted Ph; R2 = (un)substituted cycloalk(en)yl, -heterocyclyl, -aryl, etc.; Z = (4-alkyl)-2-oxazoline-2,5-diyl or 4,4-dialkyl-2-oxazoline-2,5-diyl] were prepared Thus, 3,4,5-trimethoxybenzaldehyde was condensed with MeNO2 and the reduced product amidated by 4-(Me2N)C6H4COCl to give, after cyclization, I [R = C6H2(OMe)3-3,4,5, R2 = C6H4(NMe2)-4, Z = 2-oxazoline-2,5-diyl]. Data for biol. activity of I were given. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).HPLC of Formula: 256935-86-1

The Article related to oxazoline preparation antiproliferative agent, antitumor agent oxazoline preparation, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.HPLC of Formula: 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On March 15, 2005, Mavunkel, Babu J.; Chakravarty, Sarvajit; Perumattam, John J.; Dugar, Sundeep; Lu, Qing; Liang, Xi published a patent.Recommanded Product: 256935-86-1 The title of the patent was Preparation of indolylcarboxamide derivatives as inhibitors of p38 kinase. And the patent contained the following:

Title compounds I [X independently = CA, CR4A, CR5, CR52, NR6, or N; L1 = CO, SO2, or alkylene; L2 = (un)substituted-alkylene or -alkenylene; Ar = (un)substituted aryl group with substituents consisting of alkyl, alkenyl, halo, CN, etc.; Z = N or CR7 wherein R7 = H or non-interfering substituent; R1 = H, alkyl, alkenyl, alkynyl, aryl, arylalkyl, etc.; R2 independently = halo, alkyl, OH, alkoxy, etc.; R3 independently = CN, CF3, NO2, alkyl, aryl, acyl, etc.; R4 = H, halo, alkyl or alkenyl; R5 independently = H, halo, alkyl, OH, etc.; R6 = H, alkyl, alkenyl, aryl, acyl, aroyl, etc.; A = -WiCOXjY wherein Y is COR8 wherein R8 = H, (un)substituted-alkyl, -alkenyl, -alkynyl, etc.; W and X = (un)substituted-alkylene, -alkenylene, -alkynylene; Y = tetrazole, 1,2,3-triazole, 1,2,4-triazole, or imidazole and each of i and j independently = 0 or 1; m = 0-4; n = 0-3], and their pharmaceutically acceptable salts are prepared and disclosed as useful for treatment of rheumatoid arthritis. Thus, e.g., II, was prepared by carbonylation of 6-methoxy-(4-benzylpiperidinyl)-indole-5-carboxamide with oxalyl chloride and subsequent amination using 4-methylpiperazine. ELISA assays for evaluation of inhibition of p38 kinase by I revealed that all compounds of the invention possessed IC50 values in the range of 0.1-1.5 μM. I as inhibitors of p38 kinase should prove useful in the treatment of rheumatoid arthritis. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Recommanded Product: 256935-86-1

The Article related to indolylcarboxamide derivative preparation p38 kinase inhibitor antirheumatic agent, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On June 6, 2002, Dugar, Sundeep; Mavunkel, Babu J.; Luedtke, Gregory R.; Mcenroe, Glen published a patent.Formula: C9H6ClNO2 The title of the patent was Preparation of indolecarboxamides as p38-α inhibitors. And the patent contained the following:

Title compounds were prepared as p38-α inhibitors (no data). Thus, 6-chloro-1-methyl-1H-indole-5-carboxylic acid was amidated by (R)-3-aminomethyl-1-benzylpyrrolidine followed by acylation and amidation to give title compound I. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).Formula: C9H6ClNO2

The Article related to indolecarboxamide preparation p38alpha inhibitor, antiinflammatory indolecarboxamide preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Formula: C9H6ClNO2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

On March 26, 2007, Chen, Yihui; Shibata, Masayuki; Rajeswaran, Manju; Srikrishnan, Thamarapu; Dugar, Sundeep; Pandey, Ravindra K. published an article.HPLC of Formula: 256935-86-1 The title of the article was Utility of Japp-Klingemann reaction for the preparation of 5-carboxy-6-chloroindole via Fischer indole protocol. And the article contained the following:

5-Carboxy-6-chloroindole, a precursor for p38 kinase inhibitor, was prepared from 4-amino-2-chloro-3-iodobenzoic acid by following the Japp-Klingemann synthetic approach. The structures of the key intermediates were also confirmed by X-ray analyses. Computational anal. was helpful in understanding the importance of the substituents at the cyclization step of the synthesis. The experimental process involved the reaction of 6-Chloro-1H-indole-5-carboxylic acid(cas: 256935-86-1).HPLC of Formula: 256935-86-1

The Article related to carboxychloroindole preparation japp klingemann reaction, indolecarboxylic acid chloro preparation japp klingemann reaction, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.HPLC of Formula: 256935-86-1

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles