期刊
SCIENTIFIC REPORTS
卷 10, 期 1, 页码 -出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/s41598-020-63605-4
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资金
- SERB, New Delhi [CRG/2018/002159]
- CSIR, New Delhi [02(0310)/17/EMR-II]
- CSIR [09/677(0033)/2018-EMR-I]
Novel derivatives possessing imidazo[1,2-a]pyrazine and 1H-benzo[d]imidazole scaffolds were synthesized using Suzuki-Miyaura cross-coupling reactions. In vitro anticancer activities against NCI-60 cancer cell panels were tested at 10 mu M concentration. The best results were obtained from substitution of two 1-cyclohexyl-1H-benzo[d]imidazole groups present at C-6 and C-8 positions of imidazo[1,2-a]pyrazine (31). Compound 31 was found to be cytotoxic against 51 cell lines and cytostatic against 8 cell lines with broad range of growth inhibitions (-98.48 to 98.86%). GI(50) value of compound 31 was found in the range of 0.80-2.87 mu M for 59 human cancer cell lines at five-dose concentration levels. DNA binding study of potent compound 31 was suggested that this compound was intercalated into DNA base pairs with binding constant of 1.25 x 10(4)M(-1). Compound 31 showed effective binding with bovine serum albumin (BSA) and presented binding constant value of 3.79 x10(4)M(-1). Pharmacokinetic studies revealed that all compounds are following Lipinski's rule of five and expected to be orally active.
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