Abstract:Nine new chromonylthiazolidine derivatives were successfully semi-synthesized from paeonol. All of the compounds, including starting materials, the intermediate compound and products, were evaluated for their cytotoxic effects toward eight human cancer cell lines. The synthesized chromonylthiazolidines displayed weak cytotoxic effects against the tested cancer cell lines, but selective cytotoxic effects were observed. Compounds 3a and 3b showed the most selective cytotoxic effects against human epidermoid carc… Show more
“…Anh et al [ 34 ] designed a chain of novel chromony thiazolidinediones derived from knoevenagel condensation reaction between 3-formyl-7-methoxy chromone with different thiazolidinedione derivatives as presented in Scheme 25 . These synthesized derivatives were screened for their cytotoxic activity against Hep-G 2 (heptocellular carcinoma), HC-60 (acute promyeloid carcinoma), KB (epidermoid carcinoma), LLC (lewis lung carcinoma), LNCaP (hormone dependent prostate carcinoma), MCF-7 (breast cancer), SW-480 (colon adenocarcinoma) cell lines using the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2 H -tetrazolium bromide] assay.…”
Section: Biological Activities Of Thiazolidinediones Derivatives In Tmentioning
confidence: 99%
“…In this series compounds 80 , 81 and 82 showed highest cytotoxic activity against cancer cell lines. The results of potent compounds are presented in Table 26 (Anh et al [ 34 ]). Scheme 25 Synthesis of 5-((7-Methoxy-4-oxo-4 H -chromen-3-yl)methylene) substituted thiazolidine-2,4-dione …”
Section: Biological Activities Of Thiazolidinediones Derivatives In Tmentioning
Thiazolidinediones are sulfur containing pentacyclic compounds that are widely found throughout nature in various forms. Thiazolidinedione nucleus is present in numerous biological compounds, e.g., anti-malarial, antimicrobial, anti-mycobacterium, anticonvulsant, antiviral, anticancer, anti-inflammatory, antioxidant, anti-HIV (human immunodeficiency virus) and antitubercular agent. However, owing to the swift development of new molecules containing this nucleus, many research reports have been generated in a brief span of time. Therefore seems to be a requirement to collect recent information in order to understand the current status of the thiazolidinedione nucleus in medicinal chemistry research, focusing in particular on the numerous attempts to synthesize and investigate new structural prototypes with more effective antidiabetic, antimicrobial, antioxidant, anti-inflammatory, anticancer and antitubercular activity.
“…Anh et al [ 34 ] designed a chain of novel chromony thiazolidinediones derived from knoevenagel condensation reaction between 3-formyl-7-methoxy chromone with different thiazolidinedione derivatives as presented in Scheme 25 . These synthesized derivatives were screened for their cytotoxic activity against Hep-G 2 (heptocellular carcinoma), HC-60 (acute promyeloid carcinoma), KB (epidermoid carcinoma), LLC (lewis lung carcinoma), LNCaP (hormone dependent prostate carcinoma), MCF-7 (breast cancer), SW-480 (colon adenocarcinoma) cell lines using the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2 H -tetrazolium bromide] assay.…”
Section: Biological Activities Of Thiazolidinediones Derivatives In Tmentioning
confidence: 99%
“…In this series compounds 80 , 81 and 82 showed highest cytotoxic activity against cancer cell lines. The results of potent compounds are presented in Table 26 (Anh et al [ 34 ]). Scheme 25 Synthesis of 5-((7-Methoxy-4-oxo-4 H -chromen-3-yl)methylene) substituted thiazolidine-2,4-dione …”
Section: Biological Activities Of Thiazolidinediones Derivatives In Tmentioning
Thiazolidinediones are sulfur containing pentacyclic compounds that are widely found throughout nature in various forms. Thiazolidinedione nucleus is present in numerous biological compounds, e.g., anti-malarial, antimicrobial, anti-mycobacterium, anticonvulsant, antiviral, anticancer, anti-inflammatory, antioxidant, anti-HIV (human immunodeficiency virus) and antitubercular agent. However, owing to the swift development of new molecules containing this nucleus, many research reports have been generated in a brief span of time. Therefore seems to be a requirement to collect recent information in order to understand the current status of the thiazolidinedione nucleus in medicinal chemistry research, focusing in particular on the numerous attempts to synthesize and investigate new structural prototypes with more effective antidiabetic, antimicrobial, antioxidant, anti-inflammatory, anticancer and antitubercular activity.
“…Anh and colleagues [130] synthesized a new range of hybrid thiazolidine compounds attached with the naturally occurring paeonol. The compounds exhibited selective anticancer activity against eight cancer cell lines, HepG2, acute promyeloidleukemia, KB, LU-1 (human lung cancer), LLC, SW480 (colon adenocarcinoma), hormone-dependent prostate cancer and MCF7 (breast cancer) using MTT assay.…”
Section: Scheme 71 Synthesis Of Thiazolidine Derivatives 88a-dmentioning
In past decades, interdisciplinary research has been of great interest for scholars. Thiazolidine motifs behave as a bridge between organic synthesis and medicinal chemistry and compel researchers to explore new drug candidates. Thiazolidine motifs are very intriguing heterocyclic five-membered moieties present in diverse natural and bioactive compounds having sulfur at the first position and nitrogen at the third position. The presence of sulfur enhances their pharmacological properties, and, therefore, they are used as vehicles in the synthesis of valuable organic combinations. They show varied biological properties viz. anticancer, anticonvulsant, antimicrobial, anti-inflammatory, neuroprotective, antioxidant activity and so on. This diversity in the biological response makes it a highly prized moiety. Based on literature studies, various synthetic approaches like multicomponent reaction, click reaction, nano-catalysis and green chemistry have been employed to improve their selectivity, purity, product yield and pharmacokinetic activity. In this review article, we have summarized systematic approaches for the synthesis of thiazolidine and its derivatives, along with their pharmacological activity, including advantages of green synthesis, atom economy, cleaner reaction profile and catalyst recovery which will help scientists to probe and stimulate the study of these scaffolds.
“…The N–C–S linkage had been found to be responsible, in active compounds, for exhibiting antimicrobial [ 3 , 4 , 5 ] and anti-HIV [ 6 , 7 ] activities. The thiazolidine nucleus, notably 1,4-thiazolidinedione (TZD), has been widely employed as a unique scaffold in developing new potent anticancer agents showing cytotoxicity against different human cancer cells [ 8 , 9 , 10 ] and recently was intensified as a novel onset in cancer chemotherapy [ 11 , 12 ]. Efatutazone, netoglitazone, rosiglitazone and troglitazone, having the thiazolidine system in their basic skeleton, are being studied regarding the mechanism underlying their anticancer activity [ 11 ].…”
New 1-thia-azaspiro[4.5]decane derivatives, their derived thiazolopyrimidine and 1,3,4-thiadiazole compounds were synthesized. The thioglycoside derivatives of the synthesized (1,3,4-thiadiazolyl)thiaazaspiro[4.5]decane and thiazolopyrimidinethione compounds were synthesized by glycosylation reactions using acetylated glycosyl bromides. The anticancer activity of synthesized compounds was studied against the cell culture of HepG-2 (human liver hepatocellular carcinoma), PC-3 (human prostate adenocarcinoma) and HCT116 (human colorectal carcinoma) cell lines and a number of compounds showed moderate to high inhibition activities.
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