Antitumor agents. 271: Total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents

Background: Tubulysins, linear tetrapeptides show extraordinary cytotoxicity against various cancer cells, with IC50 values in nano or picomolar range. Due to their extremely vigorous anti-proliferative and antiangiogenic characteristics, tubulysins exhibit captivating prospects in the development of anticancer drugs. This review focuses on diverse routes for the total synthesis of natural and synthetic tubulysins as well as their fragments. Objective: The purpose of this review is to present the synthetic strategies for the development of antitumor agents, tubulysins. Conclusion: A range of synthetic pathways adopted for the total synthesis of tubulysins and their fragments have been described in this review. Synthesis of fragments, Tuv, Tup, and Tut can be accomplished by adopting appropriate strategies such as Manganese-mediated synthesis, Ireland-Claisen rearrangement, Mukaiyama aldol reaction, and Mannich process etc. Tubulysin B, D, U, V, and N14-desacetoxytubulysin H have been prepared through Mitsunobu reaction, tert-butanesulfinamide method, Tandem reaction, aza-Barbier reaction, Evans aldol reaction, and C-H activation strategies etc. The remarkable anticancer potential of tubulysins toward a substantiate target make them prominent leads for developing novel drugs against multidrug-resistant cancers.

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Antitumor agents. 258. Syntheses and evaluation of dietary antioxidant—taxoid conjugates as novel cytotoxic agents

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2007.06.083 ◽

2007 ◽

Vol 17 (18) ◽

pp. 5204-5209 ◽

Cited By ~ 33

Author(s):

Kyoko Nakagawa-Goto ◽

Koji Yamada ◽

Seikou Nakamura ◽

Tzu-Hsuan Chen ◽

Po-Cheng Chiang ◽

...

Keyword(s):

Antitumor Agents ◽

Cytotoxic Agents ◽

Dietary Antioxidant

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Crotonkinins A and B and Related Diterpenoids fromCroton tonkinensisas Anti-inflammatory and Antitumor Agents

Journal of Natural Products ◽

10.1021/np070383f ◽

2007 ◽

Vol 70 (12) ◽

pp. 1906-1909 ◽

Cited By ~ 27

Author(s):

Ping-Chung Kuo ◽

Yuh-Chiang Shen ◽

Mei-Lin Yang ◽

Su-Hui Wang ◽

Tran Dinh Thang ◽

...

Keyword(s):

Antitumor Agents ◽

Anti Inflammatory

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PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i6.17343 ◽

2017 ◽

Vol 10 (6) ◽

pp. 237 ◽

Cited By ~ 1

Author(s):

Ishwar Bhat K ◽

Abhishek Kumar

Keyword(s):

Acetic Acid ◽

Cytotoxic Activity ◽

Glacial Acetic Acid ◽

Antimalarial Activity ◽

Biological Activities ◽

Cytotoxic Agents ◽

Pyrimidine Derivatives ◽

Pharmacological Activities ◽

Anti Inflammatory ◽

Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

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ChemInform Abstract: Antitumor Agents. Part 209. Pheophorbide-a Derivatives as Photo-Independent Cytotoxic Agents.

ChemInform ◽

10.1002/chin.200220086 ◽

2010 ◽

Vol 33 (20) ◽

pp. no-no

Author(s):

Prapai Wongsinkongman ◽

Arnold Brossi ◽

Hui-Kang Wang ◽

Kenneth F. Bastow ◽

Kuo-Hsiung Lee

Keyword(s):

Antitumor Agents ◽

Cytotoxic Agents ◽

Pheophorbide A

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Total synthesis and biological evaluation of viscolin, a 1,3-diphenylpropane as a novel potent anti-inflammatory agent

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2006.09.046 ◽

2006 ◽

Vol 16 (24) ◽

pp. 6155-6160 ◽

Cited By ~ 22

Author(s):

Chung-Ren Su ◽

Yuh-Chiang Shen ◽

Ping-Chung Kuo ◽

Yann-Lii Leu ◽

Amooru G. Damu ◽

...

Keyword(s):

Total Synthesis ◽

Biological Evaluation ◽

Inflammatory Agent ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation

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Total synthesis and biological evaluation of seven new anti-inflammatory oxacyclododecindione-type macrolactones

Organic & Biomolecular Chemistry ◽

10.1039/d0ob00958j ◽

2020 ◽

Vol 18 (30) ◽

pp. 5906-5917

Author(s):

Carina Weber ◽

Nina Vierengel ◽

Thorsten Walter ◽

Torsten Behrendt ◽

Tobias Lucas ◽

...

Keyword(s):

Total Synthesis ◽

Inhibitory Activity ◽

Biological Evaluation ◽

Signalling Pathways ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation

Seven new macrolactones of the oxacyclododecindione family have been synthesized and tested for their inhibitory activity on TGF-β-inducible Smad2/3- as well as IL-4-inducible STAT6-dependent signalling pathways.

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Screening of Antibacterial, Thrombolytic, Membrane Stabilizing, Anti-inflammatory and Antitumor Activity of Citrus assamensis Leaf Extracts

Journal of Scientific Research ◽

10.3329/jsr.v10i2.35410 ◽

2018 ◽

Vol 10 (2) ◽

pp. 195-210

Author(s):

M. Shahriar ◽

M. A. Bhuiyan ◽

M. S. Rana

Keyword(s):

Antitumor Activity ◽

Antitumor Agents ◽

Chloroform Extract ◽

Haemolytic Activity ◽

Hypotonic Solution ◽

Leaf Extracts ◽

Thrombolytic Activity ◽

Anti Inflammatory

The methanol, ethanol and chlorofom leaf extracts of Satkara, Citrus assamensis (family: Rutaceae), were subjected to in vitro anti-bacterial, thrombolytic, membrane stabilizing and in vivo anti-inflammatory and antitumor activity tests. The chloroform extract of C. assamensis showed the most important spectrum of activity against Bacillus subtilis, Bacillus cereus, Sarcina lutea among 6 gram positive and against 11 gram negative bacteria at the concentration of 1000 μg/disc, while the range of zones of inhibition were within 7-16 mm. Among the tested three extracts CHCl3 extract showed potent thrombolytic activity and hypotonic solution induced haemolytic activity where the percentages of inhibition were found to be 35% and 55% respectively. All the extracts established significant (p<0.05) anti-inflammatory effect by regulating biphasic inflammatory process induced by carrageenan. The leaf extract dose-dependently and significantly decreases the number of EAC cell count and inhibition of cell growth in comparison to the EAC control and standard. The results obtained in the present study indicate that, C. assamensis leaf can be a potential source of anti-bacterial, thrombolytic, membrane stabilizing, anti-inflammatory and antitumor agents.

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