Potent anti-cancer drug

Hepatocellular carcinoma (HCC) is the most common primary liver malignancy and is a leading cause of cancer-related death worldwide. However, there is no effective chemotherapeutic treatment for HCC and its prognosis remains poor. Consequently, it is urgent to find an efficient antitumor agent to treat HCC. In this study, 7-ethyl-10- hydroxycamptothecin (SN38), the bioactive metabolite of the anticancer drug irinotecan (CPT-11), which is 100–1000 times more potent than CPT-11, was coupled with aspirin to give 4 prodrugs. Their structures were characterized by 1H NMR and elemental analysis.

11p tudichquannguyet 29-11-2021 12 2   Download

Quantitative structure–activity relationship (QSAR) analysis of 28 quinoline-arylamidine (CQArA) hybrids against two leukemia cells, K562 and Raji, was performed. Multiple linear regression (MLR) models were obtained by genetic algorithm. The best models involved the following descriptors: radial distribution function (RDF) descriptors, GETAWAY (GEometry, Topology, and Atom-Weights AssemblY) descriptor, bond information content index, and dipole moment. The best MLR models for K562 and Raji cells demonstrated satisfactory stability in internal and external validation.

16p tudichquannguyet 29-11-2021 7 1   Download

Expression and activity of heparanase, an endoglycosidase that cleaves heparan sulfate (HS) side chains of proteoglycans, is associated with progression and poor prognosis of many cancers which makes it an attractive drug target in cancer therapeutics.

14p vimale2711 21-08-2020 11 1   Download

Cancer is one of the leading causes of death and globally the numbers of cases of cancer are increasing gradually. There are several medicines available in the market to treat the various types of cancer but no drug is found to be fully effective and safe. The major problem in the cancer chemotherapy is the toxicity of the established drugs. However natural products have proved effective and safe in the treatment and management of cancers. These days most of the research work on cancer drugs is targeted on bio based natural products.

11p gaocaolon5 14-06-2020 10 1   Download

An efficient and a novel approach for the synthesis of some novel pyrazole based-azoles are described via multi-component reaction under controlled microwave heating conditions.

12p vijiraiya2711 27-05-2020 17 1   Download

Natural products are increasingly being considered ‘‘critical and important’’ in drug discovery paradigms as a number of them such as camptothecin, penicillin, and vincristine serve as ‘‘lead molecules’’ for the discovery of potent compounds of therapeutic interests namely irinotecan, penicillin G, vinblastine respectively. Derived compounds of pharmacological interests displayed a wide variety of activity viz. anticancer, anti-inflammatory, antimicrobial, anti-protozoal, etc.; when modifications or derivatizations are performed on a parent moiety representing the corresponding derivatives.

9p trinhthamhodang1 16-11-2019 15 1   Download