Synthesis, Biological Evaluation and In Silico Studies of Certain Oxindole-Indole Conjugates as Anticancer CDK Inhibitors.

ABSTRACT: On account of their overexpression in a wide range of human malignancies, cyclin-dependent kinases (CDKs) are among the most validated cancer targets, and their inhibition has been featured as a valuable strategy for anticancer drug discovery. In this study, a hybrid pharmacophore approach was adopted to develop two series of oxindole-indole conjugates (6a-i and 9a-f) and carbocycle-indole conjugates (11a,b) as efficient antitumor agents with potential inhibitory action toward CDK4. All oxindole-indole conjugates, except 6i, 9b, and 9c efficiently affected the growth of the human breast cancer MCF-7 (IC₅₀: 0.39 ± 0.05-21.40 ± 1.58 μM) and/or MDA-MB-231 (IC₅₀: 1.03 ± 0.04-22.54 ± 1.67 μM) cell lines, whereas bioisosteric

SUBMITTER: Al-Warhi T 

PROVIDER: S-EPMC7248897 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature