Synthesis and antitumor activity of aromatic camptothecin esters.

T1 - Synthesis and antitumor activity of structural analogues of the epipodophyllotoxins

Synthesis and Antitumor Activity of a New Ergosterol Derivative

T1 - Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors

Total Synthesis of Potential Antitumor Agent, (−)-Dictyostatin

In the 1920s, the Nobel Prize winner Otto Warburgobserved a marked increase in glycolysis and enhanced lactateproduction in tumor cells even when maintained in conditions ofhigh oxygen tension (termed Warburg effect), leading to widespreadconcerns about the metabolic changes in human types of cancer(). Either as a consequence or asa cause, alterations of cancer cell-intrinsic metabolism have beenconsidered as essential hallmarks of cancer. Among these metabolicchanges, fatty acid biosynthesis was found elevatedin the majority of human types of cancer, such as prostate(), colorectal (), ovarian (), bladder (), esophageal (), gastric (), lung (), endometrial (), breast () and soft tissue sarcomas (). Fatty acid synthase (FASN) isregarded as a key regulator of fatty acid synthesisand was widely found upregulated in a wide variety of humanmalignancies and their pre-neoplastic lesions. Recent studies alsoreveal that FASN is associated with the stage of cancer andindicate a poor prognosis ().Thus, FASN could be considered as a reliable predictor ofrecurrence and disease-free survival along with neo-plastic stage(). treatmentwith inhibitors of FASN has been proven to lead to markedlydecreased survival in human cancer xenografts () and silencing of the FASN gene bysiRNA also inhibits cancer cell growth and ultimately inducescancer cell apoptosis ().Therefore, agents that inhibit FASN and the fatty-acid synthesis pathways could be considered as novelantitumor strategies.

C9-Substituted phenanthrene-based tylophorine derivatives (PBTs) (13-36) were synthesized and evaluated as in vitro anticancer agents against the human A549 lung cancer cell line. Twelve active compounds were further examined against DU-145 (prostate), ZR-751 (breast), KB (nasopharyngeal), and KB-Vin (multidrug resistant KB subline) human cancer cell lines. They showed potent cytotoxic activity against both wild type and matched multidrug resistant KB cell lines, and displayed notable selectivity toward DU-145 (prostate) and ZR-751 (breast) cancer cell lines. The mode of action of this class may be distinctly different from that of other cancer chemotherapeutic compounds. Three PBT analogs were also evaluated in a murine model. Compound 24b showed modest in vivo antitumor activity against human A549 xenograft in nude mice as well as potent in vitro cytotoxic activity, and thus, is a promising anticancer lead compound.


Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs

Wang Y, Jin J, Zhu L, Zhang Y, Chen X, Gao X, et al. Synthesis and anti tumor activity of novel 2-(1-substitutedpiperdin-4-ylamino) quinazolines as antitumor agents. Acta Pharmaceutica Sinica 2012; 47; 1164-78.

Synthesis and antitumor activity of 1,2,4-triazoles …

Cai J, Sun M, Wu X, Chen J, Wang P, Zong X, et al. Design and synthesis of novel 4-benzothiazole amino quinazolines dasatinib derivatives as potential anti-tumor agents. Eur J Med Chem 2013; 63: 7002-12.

Photo-induced synthesis and in vitro antitumor activity of ..

Al-Obaid AM, Abdel-Hamide SG, El-Kashef HA, Alaa AM, El-Azab AS, Al-Khamees HA, et al. Substituted quinazolines, part 3. Synthesis, in vitro antitumor activity and molecular modeling study of certain 2-thieno-4 (3H)-quinazolinone analogs. Eur J Med Chem 2009; 44: 2379-91.

Synthesis and antitumor activity of camptothecin-20-O …

Sarah TAR, Ihsan AA, Mahmoud NN, Laila AA, Alaa AMA, Sami GA, et al. Synthesis, dihydrofolate reductase inhibition, antitumor testing, and molecular modeling study of some new 4 (3H)-quinazolinone analogs. Bioorg Med Chem 2006; 14(24): 8608-21.

Synthesis, characterization, and antitumor activity of …

Sathisa MP, Revankar VK, Pai KSR. Synthesis, structure, electro chemistry and spectral characterization of bis-isatin thiocarbohydrazone metal complexes and their antitumor activity against ehrlich ascites carcinoma in swiss albino mice. Met based drugs 2007; 2008: 1-11.