Synthesis and anticancer activity of some novel fused pyridine ring system

Abstract

New series of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines (7a,b) and thieno[2,3-b:4,5-b'] dipyridine (11a-c) were synthesized from 4-aryl-6-(4-chlorophenyl)-2-thioxo-1,2-dihydro pyridine-3-carbonitriles 4a,b via application of Thorpe-Zielger reaction. The novel target compounds were evaluated in vitro for their anticancer activity against human breast adenocarcinoma MCF-7 and colon carcinoma cell line (HCT 116). Most of the tested compounds exploited potent to moderate growth inhibitory activity, in particular compound 11d, which exhibited superior potency to the reference drug Doxorubicin (IC(50) = 5.95, 6.09 and 8.48, 8.15 μM, respectively). The structures of the compounds obtained were determined by spectroscopic data.

Design and synthesis of new series of 3‐cyanopyridine and pyrazolopyridine derivatives

“…Pyridine is one of the most popular moieties incorporated into the structure of wide range of biologically active compounds. Among these, cyanopyridines (nicotinonitriles) have various biological activities, as antimicrobial [8][9][10], anticancer [10][11], antihypertensive [12], analgesic, antipyretic, anti-inflammatory [13][14][15], antioxidant [16][17][18][19], anti-Alzheimer [20], and anticonvulsant [21]. On the other hand, some nicotinonitrile derivatives are used as electrical materials [22] and optical materials [23].…”

A Review: Synthesis and Medicinal Importance of Nicotinonitriles and Their Analogous

“…Pyridine is one of the most popular N ‐heteroaromatics incorporated into the structure of many pharmaceuticals. Among these, cyanopyridines (nicotinonitriles) that, have been found therapeutic activities of biological activities, such antimicrobial , anticancer , antihypertensive , anti‐inflammatory, analgesic, and antipyretic properties . Furthermore, some nicotinonitrile derivatives are used as nonlinear optical materials and electrical materials .…”

A Green Synthesis of 7‐amino‐5‐(4‐aroyl)‐1,3‐dimethyl‐2,4‐dioxo‐1,2,3,4,5,8‐hexahydropyrido[2,3‐d]pyrimidine‐6‐carbonitrile Derivatives by a One‐pot Three‐component Reaction

“…Recently, the pyrido[2,3‐ d ]pyrimidine derivatives have received considerable attention because of their biological and pharmacological activities such as anti‐AIDS , antifungal , antileishmanial , tuberculostatic , antimicrobial , antitumor , tyrosin ekinase , anti‐inflammatory , antiallergic , analgesic , antibronchitic , hepatoprotective , antihypertensive , calcium channel antagonists , and antibacterial .…”