Recommanded Product: 123-11-5. Authors Nagy, MI; Darwish, KM; Kishk, SM; Tantawy, MA; Nasr, AM; Qushawy, M; Swidan, SA; Mostafa, SM; Salama, I in MDPI published article about in [Nagy, Manar, I; Darwish, Khaled M.; Kishk, Safaa M.; Mostafa, Samia M.; Salama, Ismail] Suez Canal Univ, Fac Pharm, Dept Med Chem, Ismailia 41522, Egypt; [Tantawy, Mohamed A.] Natl Res Ctr, Hormones Dept, Med Res Div, Giza 12622, Egypt; [Nasr, Ali M.] Port Said Univ, Fac Pharm, Dept Pharmaceut, Port Said 42526, Egypt; [Nasr, Ali M.; Qushawy, Mona] Sinai Univ, Fac Pharm, Dept Pharmaceut, Alarish 45511, North Sinai, Egypt; [Qushawy, Mona] Univ Tabuk, Fac Pharm, Dept Pharmaceut, Tabuk 71491, Saudi Arabia; [Swidan, Shady A.] British Univ Egypt, Fac Pharm, Dept Pharmaceut, Cairo 11837, Egypt; [Swidan, Shady A.] British Univ Egypt, Fac Pharm, Ctr Drug Res & Dev CDRD, Cairo 11837, Egypt in 2021.0, Cited 90.0. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
Cancer is a multifactorial disease necessitating identification of novel targets for its treatment. Inhibition of Bcl-2 for triggered pro-apoptotic signaling is considered a promising strategy for cancer treatment. Within the current work, we aimed to design and synthesize a new series of benzimidazole- and indole-based derivatives as inhibitors of Bcl-2 protein. The market pan-Bcl-2 inhibitor, obatoclax, was the lead framework compound for adopted structural modifications. The obatoclax’s pyrrolylmethine linker was replaced with straight alkylamine or carboxyhydrazine methylene linkers providing the new compounds. This strategy permitted improved structural flexibility of synthesized compounds adopting favored maneuvers for better fitting at the Bcl-2 major hydrophobic pocket. Anti-cancer activity of the synthesized compounds was further investigated through MTT-cytotoxic assay, cell cycle analysis, RT-PCR, ELISA and DNA fragmentation. Cytotoxic results showed compounds 8a, 8b and 8c with promising cytotoxicity against MDA-MB-231/breast cancer cells (IC50 = 12.69 +/- 0.84 to 12.83 +/- 3.50 mu M), while 8a and 8c depicted noticeable activities against A549/lung adenocarcinoma cells (IC50 = 23.05 +/- 1.45 and 11.63 +/- 2.57 mu M, respectively). The signaling Bcl-2 inhibition pathway was confirmed by molecular docking where significant docking energies and interactions with key Bcl-2 pocket residues were depicted. Moreover, the top active compound, 8b, showed significant upregulated expression levels of pro-apoptotic/anti-apoptotic of genes; Bax, Bcl-2, caspase-3, -8, and -9 through RT-PCR assay. Improving the compound’s pharmaceutical profile was undertaken by introducing 8b within drug-solid/lipid nanoparticle formulation prepared by hot melting homogenization technique and evaluated for encapsulation efficiency, particle size, and zeta potential. Significant improvement was seen at the compound’s cytotoxic activity. In conclusion, 8b is introduced as a promising anti-cancer lead candidate that worth future fine-tuned lead optimization and development studies while exploring its potentiality through in-vivo preclinical investigation.
Recommanded Product: 123-11-5. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Nagy, MI; Darwish, KM; Kishk, SM; Tantawy, MA; Nasr, AM; Qushawy, M; Swidan, SA; Mostafa, SM; Salama, I or concate me.
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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