Design, Synthesis and SAR Study of Novel Spiro [Pyrimido[5, 4‐b]Quinoline‐10, 5′‐Pyrrolo[2, 3‐d]Pyrimidine] Derivatives as Promising Anticancer Agents. (13th August 2018)

• Record Type: Journal Article
• Authors: Chate, Asha V.; Kamdi, Sagar P.; Bhagat, Amruta N.; Jadhav, Chetan K.; Nipte, Amol; Sarkate, Aniket P.; Tiwari, Shailee V.; Gill, Charansingh H.
• Is Part Of: Journal of heterocyclic chemistry. Volume 55:Number 10(2018)
• Page Start: 2297
• Page End: 2302
• Publication Date: 2018-08-13
• Subjects: Heterocyclic compounds -- Periodicals; 547.59
• DOI: 10.1002/jhet.3286
• Languages: English
• ISSNs: 0022-152X

Abstract

Abstract : Novel spiro [pyrimido[5, 4‐b]quinoline‐10, 5′‐pyrrolo[2, 3‐d]pyrimidine] derivatives were designed and synthesized, and their chemical structures were confirmed by IR, NMR, elemental analysis, and mass spectral analysis. The anticancer activities of the newly synthesized compounds were evaluated in vitro against four human cancer cell lines including A431, PC‐3, MCF‐7, and MCF‐10A by MTT assay. The screening results showed that three compounds (4m, 4q, and4s ) exhibited potent cytotoxic activities with IC50 values between 7.82 and 9.88 μM against human breast cancer cell line (MCF‐7). Further in vitro studies revealed that inhibition of Sunitinib could be the possible mechanism of action of these molecules. Abstract :