1666-00-8Relevant articles and documents
Studies on triepoxide analogs of triptolide
Yang, Dan,Wong, Man-Kin,Cheung, Kung-Kai,Chan,Xie, Yong
, p. 6865 - 6868 (1997)
Several triepoxide analogs of triptolide were synthesized efficiently using in situ generated dioxiranes and basic hydrogen peroxide. Two of them were found to be cytotoxic.
Synthesis of thymol-based pyrazolines: An effort to perceive novel potent-antimalarials
Raghuvanshi, Dushyant Singh,Verma, Narsingh,Singh, Shiv Vardan,Khare, Sonam,Pal, Anirban,Negi, Arvind Singh
supporting information, (2019/05/01)
A series of thymol based substituted pyrazolines and chalcones was synthesized and evaluated for antimalarial activity, using in-vitro and in-vivo malaria models. All the target compounds (5a-k and 6a-j)were found to be active against human malaria parasite strain Plasmodium falciparum NF54. Among all, compounds 5e and 5f of chalcone series and 6c and 6f of pyrazoline series exhibited prominent antimalarial activity with IC50 less than 3 and 2 μM respectively, while other pyrazolines also significantly inhibited the P. falciparum with IC50 less than 10 μM. The designed pharmacophores were found to be effective against P. falciparum. Compound 6f was found to be able to retard malaria progression in mice. This was evident through decreased parasitemia, increased mean survival time and hemoglobin content in the treated animals. Moreover, 6f was observed as an inhibitor of heme polymerization pathway of the malaria parasite. It also inhibited free heme degradation, which could be possibly responsible for higher reactive oxygen species (ROS)in parasite, thus inhibiting the rapid proliferation of the parasite. In addition to this, compound 6f was found to be non-toxic with a good selectivity index. Based on these observations, the compound 6f could be taken up for further antimalarial lead optimization studies.
Synthesis, characterizations, biological activities and docking studies of novel dihydroxy derivatives of natural phenolic monoterpenoids containing azomethine linkage
Rajput, Jamatsing D.,Bagul, Suresh D.,Hosamani, Amar A.,Patil, Manohar M.,Bendre, Ratnamala S.
, p. 5377 - 5393 (2017/09/23)
Abstract: In the present work, we report the synthesis of six new azomethine linkage containing dihydroxy derivatives of carvacrol, thymol, and eugenol. All the synthesized derivatives have been characterized by spectroscopic techniques and their structures were confirmed by X-ray single crystallography. Synthesized derivatives were screened for anti-oxidant activity using DPPH radical scavenging assay, and anticancer activity by using SRB assay against pancreatic cancer with MIAPaCa-2 and colon cancer with HCT-15 cell lines. The molecular docking studies of all the synthesized derivatives were performed on cyclooxygenases (COX-2) protein enzyme. In the anti-oxidant test, the values of EC50 indicated that all the compounds show excellent anti-oxidant potency, and similarly the GI50 values in anticancer tests indicated that most of the compounds possess good anticancer efficacy. The overall docking score suggested that all the synthesized compounds exhibit good binding affinity towards cyclooxygenases (COX-2) protein enzyme.
