2016
DOI: 10.22159/ijcpr.2017v9i1.16625
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MOLECULAR DOCKING STUDY ON 1H-(3,4d) PYRAZOLO-PYRIMIDINES AS CYCLIN DEPENDANT KINASE (CDK2) INHIBITORS

Abstract: Objective: CDK2 inhibitors are implicated in several carcinomas viz. Carcinoma of lung, bladder, sarcomas and retinoblastoma. Pyrazolopyrimidines, being purine bioisosters inhibit more than one type of kinase. In this study, we are studying some novel derivatives of 1H-pyrazolo [3,4d] pyrimidines not reported earlier. The objective of the present study is an attempt towards design and development of 1H-[3,4-] pyrazolo-pyrimidines as CDK2 inhibitors through rational drug design. Methods:The present study has b… Show more

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Cited by 5 publications
(4 citation statements)
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“…Therefore, the discovery and development of new chemical entities with a novel mechanism of action, safe and efficacious drugs, and shorter duration of treatment are the desperate needs for infectious diseases research programs. Pioneering scientists had reported pyrazole and its derivatives for an extensive range of pharmacological activities such as antipyretic, analgesic, antimicrobial, anticancer, antitubercular, antiviral, antihypertensive, antioxidant, antidepressant, and anxiolytic [5][6][7]. Rangappa S. Keri et al reviewed and discussed the possible structure-activity relationship of different types of pyrazole scaffold for designing of better antitubercular agents [8].…”
Section: Introductionmentioning
confidence: 99%
“…Therefore, the discovery and development of new chemical entities with a novel mechanism of action, safe and efficacious drugs, and shorter duration of treatment are the desperate needs for infectious diseases research programs. Pioneering scientists had reported pyrazole and its derivatives for an extensive range of pharmacological activities such as antipyretic, analgesic, antimicrobial, anticancer, antitubercular, antiviral, antihypertensive, antioxidant, antidepressant, and anxiolytic [5][6][7]. Rangappa S. Keri et al reviewed and discussed the possible structure-activity relationship of different types of pyrazole scaffold for designing of better antitubercular agents [8].…”
Section: Introductionmentioning
confidence: 99%
“…Validation of generated model using Golbraikh-Tropsha acceptance criteria, k-fold cross validation, leave one out, viii. Applicability domain analysis using Euclidean distance and Mahalanobis distance [80][81].…”
Section: Future Scopementioning
confidence: 99%
“…After that, at the G2/M phase, CDK-1 binds to cyclin B. CDK-2 activation by cyclin E is a key step for the cell cycle to progress through G1 to S phase, and this nominates CDK-2 as a major target for most anti-proliferative drugs [3,4]. CDK-2 is found to be overexpressed in a variety of human cancer as breast, ovarian, endometrial, thyroid carcinomas, lung, and osteosarcoma [4,5].…”
Section: Introductionmentioning
confidence: 99%