- PYRIDAZINONES AS PARP7 INHIBITORS
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The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.
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Paragraph 1709
(2019/11/11)
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- Serinolamides and Lyngbyabellins from an Okeania sp. Cyanobacterium Collected from the Red Sea
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NMR- and MS-guided fractionation of an extract of an Okeania sp. marine cyanobacterium, collected from the Red Sea, led to the isolation of four new metabolites, including serinolamides C (1) and D (2) and lyngbyabellins O (3) and P (4), together with the three known substances lyngbyabellins F (5) and G (6) and dolastatin 16 (7). The planar structures of the new compounds were determined using NMR and MS analyses. The absolute configurations of 1 and 2 were determined by Marfey's analysis of their hydrolysates. The absolute configuration of 3 was ascertained by chiral-phase chromatography of degradation products, while that of 4 was determined by comparison to 3 and 5. The cytotoxic and antifouling activities of these compounds were evaluated using MCF7 breast cancer cells and Amphibalanus amphitrite larvae, respectively. Compounds 3, 4, and 7 exhibited strong antifouling activity, and 3 and 7 were not cytotoxic. A structure-activity relationship was observed for the cytotoxicity of the lyngbyabellins with the presence of a side chain (4 is more active than 3) leading to greater activity. For the antifouling activity, the acyclic form without a side chain (3) was the most active.
- Petitbois, Julie G.,Casalme, Loida O.,Lopez, Julius Adam V.,Alarif, Walied M.,Abdel-Lateff, Ahmed,Al-Lihaibi, Sultan S.,Yoshimura, Erina,Nogata, Yasuyuki,Umezawa, Taiki,Matsuda, Fuyuhiko,Okino, Tatsufumi
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p. 2708 - 2715
(2017/11/06)
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- Concise synthesis of (+)-serinolamide A
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Serinolamide A, isolated from a species of marine cyanobacteria, exhibits a moderate agonist effect and selectivity for the CB1 cannabinoid receptor, which is unusual for marine natural products. Herein, we reported a highly efficient enantiospecific first total synthesis of (+)-serinolamide A from l-serine in nine steps with 30% overall yield. The synthesis method provides a facile, practicable, and economical approach for the preparation of other similar endocanabinoid lipids.
- Gao, Ya-Ru,Guo, Shi-Huan,Zhang, Zhuan-Xiang,Mao, Shuai,Zhang, Yan-Lei,Wang, Yong-Qiang
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p. 6511 - 6513
(2013/11/19)
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- First asymmetric synthesis of the antiepileptic drug Lacosamide (Vimpat) based on a hydrolytic kinetic resolution strategy
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An efficient asymmetric synthesis of the new antiepileptic drug, Lacosamide is described in high enantiopurity (>98% ee), using Jacobsen's hydrolytic kinetic resolution strategy as a key step.
- Muthukrishnan,Mujahid,Sasikumar,Mujumdar
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scheme or table
p. 1353 - 1357
(2011/11/29)
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