Cytotoxic Effects of Thiazolo[3,2-C]Pyrimidines Against Mcf-7 And Hepg2/C3a Carcinoma Cell Lines

Abstract

Ö ZÇ alışmamızda, yeni tiyazolo[3,2-c]pirimidinlerin (4,5) bir serisi, basit ve etkili bir yöntemle hazırlandı ve bu bileşiklerin in vitro sitotoksisiteleri insan meme (MCF-7) ve karaciğer (HEPG2/C3A) kanser hücre hatları üzerinde çalışıldı. In vitro çalışma sonuçları, tiyazolo[3,2-c]pirimidinlerin en az 5 tanesinin düşük derişimlerde MCF-7 ve HEPG2/C3A kanser hücre hatlarına karşı kuvvetli sitotoksik etki gösterdiğini ortaya koymaktadır ki bu etki kullanılan referans antitümör ajanın, 5-FU, etkisiyle aynı veya daha düşüktür. Anahtar KelimelerAntikanser, meme kanseri, Mannich halkalaşması, tiyazolopirimidinler. A B S T R A C TI n the present study, a series of thiazolo[3,2-c]pyrimidines (4,5) have been produced via simple and efficient synthetic method and their in vitro cytotoxicities have been performed on human breast (MCF-7) and hepatocellular (HEPG2/C3A) adenocarcinoma cell lines. The results of these in vitro tests revealed that at least five of thiazolo[3,2-c]pyrimidines exhibited strong cytotoxic effects at very low concentrations, which were very similar or lower than that of reference anticancer agent, 5-FU, against MCF-7 and HEPG2/C3A cancer cell lines.

Antiproliferative effect of indeno[1,2-d]thiazolo[3,2-a]pyrimidine analogues on IL-6 mediated STAT3 and role of the apoptotic pathway in albino Wistar rats of ethyl carbamate-induced lung carcinoma: In-silico, In-vitro, and In-vivo study

“…5-FU or 5-fluro-2, 4-pyrimidinedione is a chemotherapeutic drug frequently delivered either by a single medication or in combination with other therapeutic regimens [9][10][11][12]. 5-FU is an anticancer antimetabolite drug primarily derived from thiazolo-pyrimidines that comprise a thiazole and a pyrimidine ring, which inhibit the proliferation of cancer cells [13,14]. This has led to considerable hope for the development of new chemical moieties with pyrimidine ring.…”

Synthesis and Cytotoxic Activity of New Thiazolopyrimidine Sugar Hydrazones and Their Derived Acyclic Nucleoside Analogues

“…Thiazolopyrimidine is one of the most interesting heterocyclic scaffolds possessing structural similarity to 5-fluorouracil (5-FU)-the well-known cancer metabolite. In addition, they have been reported to possess various important potent activities such as antimicrobial, antipsychotic, anti-inflammatory, anti-Parkinson's, analgesic, antidepressant, anti-HIV, and anticancer activities [3][4][5][6][7][8][9][10][11]. In addition, they have been revealed with their bioactivities as transient receptor potential vanilloid-receptor 1 (TRPV1) modulators [12,13], antioxidants [14,15], pesticides [16], phosphate inhibitors [17,18], acetylcholinesterase inhibitors [19,20], and antimicrobial activities [21][22][23].…”