Chemistry Research Journal considers all manuscripts on the strict condition that they have not been published already, under review elsewhere, nor are they under consideration for publication or in press elsewhere. Papers not sufficiently substantiated by experimental detail will not be published. Experimental research on vertebrates or any regulated invertebrates must comply with Institutional, National, or International guidelines, and where available should have been approved by an appropriate ethics committee.
Search Medicinal Chemistry Research v. In this article, a novel series of E 3,4,5-trimethoxyphenyl acrylic acid TMCA amide derivatives were Medicinal chemistry research articles and synthesized by a facile and one-pot step, which were achieved with good yields using 1-hydroxybenzotriazole HOBT and 1- 3-Dimethylaminopropyl ethylcarbodiimide hydrochloride EDCI as activation system.
All the synthesized derivatives were biologically evaluated for their anticonvulsant, sedative activity and neurotoxicity using the maximal electroshock MES model, sc-pentylenetetrazol PTZ model, pentobarbital sodium-induced sleeping model, and locomotor activity tests, respectively.
Among them, compounds 4, 9 and 16 exhibited good anticonvulsant activity in primary evaluation. Furthermore, compound 4 is the most effective anticonvulsant and sedative agent in subsequent tests, while the low threshold of toxicity of compound 4 is vigilant. Compounds 9 and 16 also performed significantly anticonvulsant activity in subsequent tests with weak toxicity.
The molecular modeling experiments also predicted good binding interactions of the obtained active molecules with the GABA transferas. Therefore, it could be concluded that the synthesized derivatives 4, 9 and 16 would represent useful lead compounds for further investigation in the development of anticonvulsant and sedative agents.
Synthesis; 3,4,5-Trimethoxycinnamic acid; Amide derivatives; Anticonvulsant; Sedative; Docking Synthesis, cytotoxic activity, and mode of action of new Santacruzamate A analogs by Silmara N.
Evangelista; Diego Seckler; Deisielly R. Humberto; Adriano de P.
Breast and ovarian cancer are the most common cancers in women. Available cancer treatments, in general, have limited efficacy and frequent, undesirable side effects. Recently, scientists have focused on searching for new epigenetic modulators such as inhibitors of DNA methyltransferases and histone deacetylases HDACswith novel properties and selectivity.
We report the synthesis of seven new analogs of Santacruzamate A. Compound 5, the most potent and selective of the series, exhibited remarkably enhanced anticancer potency, with IC50 values for the tumor cells of Further investigation showed that compound 5 could promote DNA damage, increase the activity of caspases-3 and -9, and upregulate mRNA levels of p21, TP53, and BAK, suggesting apoptotic cell death of the tumor cells via the intrinsic pathway.
This study demonstrated that synthetic analogs of santacruzamate A with zinc-linked groups are effective for improving both HDAC inhibition and antitumor activity. Chalcones are a group of molecules with a broad spectrum of biological activities, being especially appealing for their antiproliferative effects on several cancer cell lines.
For this reason, we synthesized 23 chalcones with good to excellent yields and assessed their effect on the viability of the SH-SY5Y neuroblastoma cell line and on primary human fibroblasts. The results indicated that 18 of these compounds were more active than 5-fluorouracil in the cancer cell line and one of them was more selective than this reference drug.
To identify structural features related to the antiproliferative activity of these compounds, as well as, the selectivity on the cancer cell line, a 2D-QSAR analysis was performed. Barbosa; John Boukouvalas; Silvia H.Journal description.
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