شیمى کاربردى روز

شیمى کاربردى روز

بررسی قدرت سمیت سلولی مشتقات دی پیرولو [ c-'1،'2: a-2،1] پیرازین ها و مشتقات پیرولو [2''،1'': 3'،4 '] پیرازینو [1'،2': 5،1]پیرولو [3،2-d] پیریدازین-8 (9H)-اون‌ها

نوع مقاله : مقاله علمی پژوهشی

نویسندگان
1 دانشکده شیمی، دانشگاه سمنان، سمنان، ایران
2 گروه شیمی دارویی، دانشکده داروسازی،مرکز تحقیقات طراحی و توسعه دارو
چکیده
سرطان دومین عامل مرگ در جهان پس از بیماری‌های قلبی عروقی است. داده‌های گزارش شده توسط سازمان بهداشت جهانی (WHO) درباره این بیماری، افزایش نگران‌کننده‌ای در شیوع و مرگ و میر ناشی از این بیماری در طول دهه گذشته را نشان می‌دهد. بنابراین، تلاش‌های قابل توجهی در جهت کشف و توسعه عوامل ضد سرطان جدید و قوی صورت گرفته است. در تلاش برای یافتن و توسعه ترکیبات جدید با قدرت‌ سایتوکسیک، مسیر سنتزی موثر، ساده و چند مرحله‌ای برای تولیدمشتقاتی از دی‌هیدرو دی پیرولو[ c-'1،'2: a-2،1] پیرازین-2،3-دی کربوکسیلات 8a-8s به کار برده شدند، که پس از آن دستخوش واکنش حلقوی شدن در حضور هیدرازین هیدرات شده که منجر به تولید تتراهیدروپیرولو [2''،1'': 3'،4 '] پیرازینو [1'،2': 5،1] پیرولو [3،2-d] پیریدازین-8(9H)-اون‌ها 10a-10q شدند. سپس، سمیت سلولی آن‌ها در مقابل پنج خط سلولی سرطانی انسانی، از جمله MCF7، HeLa، SW480، HepG2 و A549 با استفاده از آزمایش رنگی MTT بررسی شد. با توجه به نتایج، ارزیابی‌های بیشتری روی ترکیب 8l انجام شد که نشان داد القای آپوپتوز و توقف چرخه سلولی G0 را در سلول‌های MCF7 و A549 رخ می‌دهد.
کلیدواژه‌ها
موضوعات

عنوان مقاله English

Investigation of the Cytotoxic Potencies of substituted dipyrrolo[1,2-a:2',1'-c]pyrazines and substituted pyrrolo[2'',1'':3',4']pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-8(9H)-ones

نویسندگان English

Azam Barghi Lish 1
Eskandar Kolvari 1
Alireza Foroumadi 2
Nadiya Koukabi 1
1 Faculty of Chemistry, Semnan University, Semnan, Iran
2 Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
چکیده English

Cancer is the world's second leading cause of death after cardiovascular diseases. The data reported by the World Health Organization (WHO) about this disease indicates a troubling increase in both prevalence and mortality over the past decade. Consequently, significant efforts have been directed toward the discovery and development of a new and potent anticancer agents. In an attempt to find and develop further new compounds possessing cytotoxic potencies, the efficient, simple, and multi-step synthetic routes were employed to afford various substituted dihydrodipyrrolo[1,2-a:2',1'-c]pyrazine-2,3-dicarboxylates 8a-8s, which were subsequently subjected to cyclization in the presence of hydrazine hydrate to produce tetrahydropyrrolo[2'',1'':3',4']pyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-8(9H)-ones 10a-10q. Afterwards, their cytotoxicity were examined against five human cancerous cell lines, including MCF7, HeLa, SW480, HepG2, and A549 by using the MTT colorimetric assay. Considering the results, further evaluations were conducted on the compound 8l, which exhibited the induction of apoptosis and G0 cell cycle arrest in MCF7 and A549 cells.

کلیدواژه‌ها English

: pyrrolo[1
2-a]pyrazine
5
6-dihydropyrrolo[1
2-a:2'
1'-c]pyrazine
cancer
N-aminoethylpyrrole
aryl glyoxal
dimethyl acetylenedicarboxylate
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