Synthesis of Some Polysubstituted Nicotinonitriles and Derived Pyrido[2,3-d]pyrimidines as In Vitro Cytotoxic and Antimicrobial Candidates
Joint Authors
Faidallah, Hassan M.
Rostom, Sherif A. F.
Khan, Khalid Ali
Source
Issue
Vol. 2016, Issue 2016 (31 Dec. 2016), pp.1-12, 12 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2016-05-15
Country of Publication
Egypt
No. of Pages
12
Main Subjects
Abstract EN
The synthesis of polysubstituted pyridines, in addition to some derived pyrido[2,3-d]pyrimidine ring systems supported with chemotherapeutically active functionalities, is described.
They were evaluated for their in vitro cytotoxic effects against three different human tumor cell lines (human colon carcinoma HT29, hepatocellular carcinoma Hep-G2, and Caucasian breast adenocarcinoma MCF7).
Nine compounds displayed variable cytotoxic potential, among which alkylthio analogs 33, 34, and 37 emerged as the most active members, being almost twice as active as doxorubicin against the colon carcinoma HT29 cell line.
In addition, the same three analogs showed a clear differential cytotoxic profile as they exhibited a marginal inhibitory effect on the growth of the normal nontransformed human foreskin fibroblast Hs27 cell line.
Meanwhile, nineteen compounds were able to exhibit significant antibacterial activity against both Gram-positive and Gram-negative bacteria, together with moderate antifungal activities.
The pyrido[2,3-d]pyrimidine-2(1H)-thione 30 together with its alkylthio derivatives 33 and 34 stemmed as the most active antimicrobial members being equipotent to ampicillin against S.
aureus, E.
coli, and P.
aeruginosa, together with a noticeable antifungal activity against C.
albicans.
Compounds 33 and 34 could be considered as a promising template for possible dual antimicrobial-anticancer candidates.
American Psychological Association (APA)
Faidallah, Hassan M.& Rostom, Sherif A. F.& Khan, Khalid Ali. 2016. Synthesis of Some Polysubstituted Nicotinonitriles and Derived Pyrido[2,3-d]pyrimidines as In Vitro Cytotoxic and Antimicrobial Candidates. Journal of Chemistry،Vol. 2016, no. 2016, pp.1-12.
https://search.emarefa.net/detail/BIM-1107575
Modern Language Association (MLA)
Faidallah, Hassan M.…[et al.]. Synthesis of Some Polysubstituted Nicotinonitriles and Derived Pyrido[2,3-d]pyrimidines as In Vitro Cytotoxic and Antimicrobial Candidates. Journal of Chemistry No. 2016 (2016), pp.1-12.
https://search.emarefa.net/detail/BIM-1107575
American Medical Association (AMA)
Faidallah, Hassan M.& Rostom, Sherif A. F.& Khan, Khalid Ali. Synthesis of Some Polysubstituted Nicotinonitriles and Derived Pyrido[2,3-d]pyrimidines as In Vitro Cytotoxic and Antimicrobial Candidates. Journal of Chemistry. 2016. Vol. 2016, no. 2016, pp.1-12.
https://search.emarefa.net/detail/BIM-1107575
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1107575