Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues.

نویسندگان

  • Bianca C Pérez
  • Iva Fernandes
  • Nuno Mateus
  • Cátia Teixeira
  • Paula Gomes
چکیده

Cinnamic acids and quinolines are known as useful scaffolds in the discovery of antitumor agents. Therefore, N-cinnamoylated analogues of chloroquine, recently reported as potent dual-action antimalarials, were evaluated against three different cancer cell lines: MKN-28, Caco-2, and MCF-7. All compounds display anti-proliferative activity in the micromolar range against the three cell lines tested, and most of them were more active than their parent drug, chloroquine, against all cell lines tested. Hence, N-cinnamoyl-chloroquine analogues are a good start towards development of affordable antitumor leads.

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

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Introducing New Antimalarial Analogues of Chloroquine and Amodiaquine: A Narrative Review

Antimalarial drugs with the 4-aminoquinoline scaffold such as the important drugs, chloroquine (CQ) and amodiaquine (AQ), have been used to prevent and treat malaria for many years. The importance of these drugs is related to their simple usage, high efficacy, affordability, and cost-effectiveness of their synthesis. In recent years, with the spread of parasite resistance to CQ and cross-resist...

متن کامل

Cryptolepine and development of new antimalarial agents

Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...

متن کامل

Cryptolepine and development of new antimalarial agents

Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...

متن کامل

ساخت آنالوگ‌های جدید 4- فلوروآمودیاکین و بررسی اثرات ضد مالاریایی دارو علیه سویه‌های حساس و مقاوم به کلروکین پلاسمودیوم فالسیپاروم

Background and Objective: Resistance to chloroquine (CQ) in Plasmodium falciparum malaria has become a major health concern in the developing countries. This problem has prompted investigators for finding alternative antimalarials that may be effective against resistant strains. Amodiaquine (AQ) is an antimalarial which is effective against many chloroquine-resistant strains of P. falciparum. H...

متن کامل

Synthesis and study of effects of new 4-chloro – amodiaquine analogues against two resistant and sensitive forms to chloroquine Plasmodium Falciparum, in vitro

Background: Resistance to chloroquine (CQ) in Plasmodium falciparum malaria has become a major health concern of the developing countries.This resistance has prompted a re-examination of the pharmacology of alternative antimalarials that may be effective against resistant strains. Amodiaquine (AQ) is a 4-aminoquinoline antimalarial which is effective against many chloroquine-resistant strains o...

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

عنوان ژورنال:
  • Bioorganic & medicinal chemistry letters

دوره 23 24  شماره 

صفحات  -

تاریخ انتشار 2013