A Comparative Study of Synthetic Approaches Towards Total Synthesis of Mandelalide A, An Anti-Lung Cancer Metabolite From Lissoclinum Ascidian

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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Recent Advances in the Total Synthesis of Clavaminols

Synthesis ◽

10.1055/s-0037-1610305 ◽

2018 ◽

Vol 50 (23) ◽

pp. 4569-4576

Author(s):

Tian Jin ◽

Lu Zhao ◽

Zhe-Bin Zheng ◽

Xiao Liu ◽

Liang Sun ◽

...

Keyword(s):

Total Synthesis ◽

Research Groups ◽

Total Syntheses ◽

New Class ◽

Recent Advances ◽

Molecular Architectures ◽

Synthetic Approaches ◽

Long Chain

Clavaminols are a new class of long-chain 2-amino-3-alkanols that mostly contain 2R,3S-configurations. Owing to their interesting molecular architectures and promising activities, they have become popular targets for synthetic organic chemists. In this review, we highlight 12 total syntheses of clavaminols from different research groups during the period 2009 to 2018.1 Introduction2 Synthetic Approaches toward Clavaminols2.1 Total Synthesis by Chemla and Colleagues (2009)2.2 Total Synthesis by Greck and Colleagues (2010)2.3 Total Synthesis by Sutherland and Zaed (2011)2.4 Total Synthesis by Huang and Colleagues (2011)2.5 Total Synthesis by Kotora and Colleagues (2012)2.6 Total Synthesis by Kumar and Colleagues (2013)2.7 Total Synthesis by Prabhavathi Devi and Colleagues (2013 and 2016)2.8 Total Synthesis by Sarabia and Colleagues (2014)2.9 Total Synthesis by Mohapatra and Colleagues (2016)2.10 Total Synthesis by Lu and Colleagues (2016)2.11 Total Synthesis by Jin and Colleagues (2017)2.12 Total Synthesis by Kumar Pandey and Colleagues (2018)3 Conclusion

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A comparative study of telomerase activity in sputum, bronchial washing and biopsy specimens of lung cancer

Lung Cancer ◽

10.1016/s0169-5002(01)00193-3 ◽

2001 ◽

Vol 33 (1) ◽

pp. 41-49 ◽

Cited By ~ 17

Author(s):

S Sen

Keyword(s):

Lung Cancer ◽

Comparative Study ◽

Telomerase Activity ◽

Biopsy Specimens ◽

Bronchial Washing

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Total Syntheses of Pladienolide-Derived Spliceosome Modulators

Molecules ◽

10.3390/molecules26195938 ◽

2021 ◽

Vol 26 (19) ◽

pp. 5938

Author(s):

Jaehoon Sim ◽

Eunbin Jang ◽

Hyun Jin Kim ◽

Hongjun Jeon

Keyword(s):

Total Synthesis ◽

Natural Product ◽

Structural Features ◽

Synthetic Approach ◽

Synthetic Analog ◽

Phase I Clinical Trials ◽

Total Syntheses ◽

Naturally Occurring ◽

Anti Cancer ◽

Synthetic Approaches

Pladienolides, an emerging class of naturally occurring spliceosome modulators, exhibit interesting structural features, such as highly substituted 12-membered macrocycles and epoxide-containing diene side chains. The potential of pladienolides as anti-cancer agents is confirmed by H3B-8800, a synthetic analog of this natural product class, which is currently under Phase I clinical trials. Since its isolation in 2004 and the first total synthesis in 2007, a dozen total syntheses and synthetic approaches toward the pladienolide class have been reported to date. This review focuses on the eight completed total syntheses of naturally occurring pladienolides or their synthetic analogs, in addition to a synthetic approach to the main framework of the natural product.

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