- Design, synthesis and biological evaluation of novel thiazole-derivatives as mitochondrial targeting inhibitors of cancer cells
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Mitochondria are pivotal energy production sources for cells to maintain necessary metabolism activities. Targeting dysfunctional mitochondrial features has been a hotspot for mitochondrial-related disease researches. Investigation with cancerous mitochondrial metabolism is a continuing concern within tumor therapy. Herein, we set out to assess the anti-cancer activities of a novel family of TPP-thiazole derivatives based on our earlier research on mitochondrial targeting agents. Specifically, we designed and synthesized a series of TPP-thiazole derivatives and revealed by the MTT assay that most synthesized compounds effectively inhibited three cancer cell lines (HeLa, PC3 and MCF-7). After structure modifications, we explored the SAR relationships and identified the most promising compound R13 (IC50 of 5.52 μM) for further investigation. In the meantime, we performed ATP production assay to assess the selected compounds inhibitory effect on HeLa cells energy production. The results displayed the test compounds significantly restrained ATP production of cancer cells. Overall, we have designed and synthesized a series of compounds which exhibited significant cytotoxicity against cancer cells and effectively inhibited mitochondrial energy production.
- Dang, Xin,Lei, Shuwen,Luo, Shuhua,Hu, Yixin,Wang, Juntao,Zhang, Dongdong,Lu, Dan,Jiang, Faqin,Fu, Lei
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- Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties
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The strong therapeutic potential of CB2 receptor agonists for use as anti-inflammatory agents that lack psychiatric side effects has attracted substantial interest. We herein describe the rational design and synthesis of novel thiazole and benzothiazole derivatives and the evaluation of their binding affinity and functional activity on CB1 and CB2 receptors. The series with the general formula N-(3-pentylbenzo [d]thiazol-2(3H)-ylidene) carboxamide (compounds 6a-6d) exhibited the highest affinity and selectivity towards CB2 receptors with Kis in the picomolar or low nanomolar range, and selectivity indices (Ki hCB1/Ki hCB2) reaching up to 429 fold. Notably, these compounds also demonstrated an agonistic functional activity in cellular assays with EC50s in the low nanomolar range. More interestingly, compound 6d, the 3-(trifluoromethyl)benzamide derivative, exhibited remarkable protection against DSS-induced acute colitis in mice model.
- Ghonim, Aya E.,Ligresti, Alessia,Rabbito, Alessandro,Mahmoud, Ali Mokhtar,Di Marzo, Vincenzo,Osman, Noha A.,Abadi, Ashraf H.
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p. 154 - 170
(2019/07/12)
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- One-Pot Telescoped Synthesis of Thiazole Derivatives from β-Keto Esters and Thioureas Promoted by Tribromoisocyanuric Acid
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A simple and efficient one-pot protocol has been developed for the synthesis of thiazole derivatives from readily available starting materials. Tribromoisocyanuric acid was successfully used for α-monohalogenation of β-keto esters in aqueous medium, which
- De Andrade, Vitor S. C.,De Mattos, Marcio C. S.
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p. 4867 - 4874
(2018/12/13)
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- A one-pot synthesis of functionalized ethyl 1,3-thiazole-5-carboxylates from thioamides or thioureas and 2-chloro-1,3-dicarbonyl compounds in an ionic liquid
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A simple one-pot synthesis of functionalized ethyl 1,3-thiazole-5- carboxylates from the reaction of 2-chloro-1,3-dicarbonyl compounds with thioureas or thioamides in the presence of 1-butyl-3-methylimidazolium trifluoromethanesulfonate is described. Grap
- Yavari, Issa,Sayyed-Alangi, S. Zahra,Hajinasiri, Rahimeh,Sajjadi-Ghotbabadi, Hadi
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experimental part
p. 209 - 211
(2010/03/26)
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- Synthesis of new substituted thiazoles containing aminooxadiazole ring
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Synthesis of biheterocyclic thiazole-amonooxadiazoles, the potential biologically active compounds is developed. Regularities of transformations and physico-chemical characteristics of intermediates and final compounds are revealed.
- Platonova,Volkova,Malin,Veretennikov,Laskin,Malin
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p. 513 - 515
(2008/09/21)
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- SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS
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The present invention relates to compounds of formula (I) or salts thereof wherein A, X and R4 are defined herein, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use
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Page/Page column 50
(2008/06/13)
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- BENZAZEPINE DERIVATIVES, PROCESS FOR THE PREPARATION OF THE SAME AND USES THEREOF
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Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally substituted hetero-alicyclic group.
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- Pyrazolecarboxylic acid derivatives and plant disease control agent
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The present invention provides a plant disease control agent containing as active ingredient one or more compounds of the formula [1]A--COOR 1 [1]whereinR 1 represents a hydrogen atom or a C 1 -C 4 alkyl group, andA represents a group of the formula (A-1) or (A-2) STR1 R 2 represents a C 1 -C 4 alkyl group, R 3 represents a C 1 -C 4 alkyl group,R 4 represents a halogen atom or a C 1 -C 4 alkyl group, andR 5 represents a C 1 -C 4 alkyl group.Further, the compound of A-1 in the formula [1] in which R 3 is a halogen atom is also included in the present invention.
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