I found the field of Biochemistry & Molecular Biology; Pharmacology & Pharmacy; Chemistry very interesting. Saw the article Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors published in 2019.0. COA of Formula: C7H8O, Reprint Addresses Tawfik, HO (corresponding author), Tanta Univ, Fac Pharm, Dept Pharmaceut Chem, El Giesh St, Tanta 31527, Egypt.. The CAS is 100-51-6. Through research, I have a further understanding and discovery of Benzyl Alcohol
A series of twenty-one 3,4-dihydropyrimidine derivatives bearing the heterocyclic 1,3-benzodioxole at position 4 in addition to different substituents at positions 2, 3 and 5 were designed and synthesized as monastrol analogs. The novel synthesized compounds were screened for their cytotoxic activity towards 60 cancer cell lines according to NCI (USA) protocol. Compounds 10b and 15 showed the best antitumor activity against most cell lines. Compound 15 was subsequently tested in 5-doses mode and displayed high selectivity towards CNS, prostate and leukemia subpanel with selectivity ratios of 22.30, 15.38 and 12.56, respectively at GI(50) level. The IC50 of compounds 9d, 10b, 12, 15 and 16 against kinesin enzyme were 3.86 +/- 0.12, 10.70 +/- 0.35, 3.95 +/- 0.12, 4.36 +/- 0.14, and 14.07 +/- 0.45 mu M respectively, while the prototype compound, monastrol, reported IC50 value of 20 +/- 0.42 mu M. The safest compound among test compounds against normal cell line (HEK 293) is 10b with IC50 value of 62.02 +/- 2.42 mu M/ml in comparison to doxorubicin (IC50 = 11.34 +/- 0.44 mu M/ml). Cell cycle analysis of SNB-75 cells treated with compound 15 showed cell cycle arrest at G2/M phase. Further, the assay of levels of active caspase-3 and caspase-9 was investigated. Moreover, Molecular docking of compounds, 9d, 10b, 12, 15, 16, monastrol and mon-97 was performed to study the interaction between inhibitors and the kinesin spindle protein allosteric binding site.
COA of Formula: C7H8O. About Benzyl Alcohol, If you have any questions, you can contact Tawfik, HO; El-Hamamsy, MH; Sharafeldin, NA; El-Moselhy, TF or concate me.
Reference:
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