Synthesis, structure-activity relationships and biological evaluation of 7-phenyl-pyrroloquinolinone 3-amide derivatives as potent antimitotic agents

نویسندگان
چکیده

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and Biological Evaluation of 2-Phenyl Benzothiazole Derivatives as Cytotoxic Agents

Cancer is a leading cause of death worldwide. Many heterocyclic cores are present in the structures of clinically approved anticancer drugs. Meanwhile, benzothiazoles have been reported as one of the most important heterocyclic scaffolds in previously reported anticancer agents in the literature. Therefore, in this report, a novel series of 2-phenyl benzothiazole derivatives was synthesized, bi...

متن کامل

Synthesis, biological evaluation and structure-activity relationships of new quinoxaline derivatives as anti-Plasmodium falciparum agents.

We report the synthesis and antimalarial activities of eighteen quinoxaline and quinoxaline 1,4-di-N-oxide derivatives, eight of which are completely novel. Compounds 1a and 2a were the most active against Plasmodium falciparum strains. Structure-activity relationships demonstrated the importance of an enone moiety linked to the quinoxaline ring.

متن کامل

Synthesis and Biological Evaluation of Amide derivatives of Benzophenone Derivatives as Anticancer Agents

A novel series of benzophenone amide derivatives (8a-j) were synthesized, and evaluated for their anticancer activity against human cancer cell lines like MCF-7, MDA MB-231(Breast cancer), A549 (Lung cancer). All the synthesized derivatives are first reported and adriamycin used as reference drug. Among the compounds, compounds 8b, 8h and 8j were showed more potent anticancer activity than cont...

متن کامل

Novel Approach Synthesis, Molecular Docking and Cytotoxic Activity Evaluation of N-phenyl-2,2-dichloroacetamide Derivatives as Anticancer Agents

Dichloroacetate (DCA) as a small, cheap and available anticancer agent, is a pyruvate mimetic compound that stimulates the activity of pyruvate dehydrogenase (PDH) enzyme through inhibition of pyruvate dehydrogenase kinases (PDHK1-4). DCA turns on programed cell death (apoptosis) which suppressed in tumor cells and therefore inhibits tumor growth. DCA also interferes with the glucose uses of ca...

متن کامل

Synthesis, biological evaluation, and structure-activity relationships of potent noncovalent and nonpeptidic cruzain inhibitors as anti-Trypanosoma cruzi agents.

The development of cruzain inhibitors has been driven by the urgent need to develop novel and more effective drugs for the treatment of Chagas' disease. Herein, we report the lead optimization of a class of noncovalent cruzain inhibitors, starting from an inhibitor previously cocrystallized with the enzyme (K(i) = 0.8 μM). With the goal of achieving a better understanding of the structure-activ...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: European Journal of Medicinal Chemistry

سال: 2017

ISSN: 0223-5234

DOI: 10.1016/j.ejmech.2016.10.026