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STEROIDS · 2014 · IF 2.716

Discovery of novel steroidal pyran–oxindole hybrids as cytotoxic agents

Bin Yu,Ping-Ping Qi,Xiao-Jing Shi,Li-Hong Shan,De-Quan Yu,Hong-Min Liu

A series of novel steroidal pyran–oxindole hybrids were efficiently synthesized in a single operation through the vinylogous aldol reaction of vinyl malononitrile 3 with substituted isatins involving the construction of C–C and C–O bonds. Some compounds displayed moderate to good cytotoxicity against T24, SMMC-7721, MCF-7 and MGC-803 cells. Compounds 4f and 4i were more potent than 5-Fu against T24 and MGC-803 cells with the IC 50 values of 4.43 and 8.45 μM, respectively. Further mechanism studies indicated that compound 4i induced G2/M arrest and early apoptosis in a concentration- and time-dependent manner.

CAS / MDL: 91-56-5

研究领域: 药物化学 · 肿瘤学 · 合成化学

✓ 已验证产品关联 DOI PubMed 高影响因子

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Frontiers in Cell and Developmental Biology · 2021 · IF 6.684

Paraquat Reduces the Female Fertility by Impairing the Oocyte Maturation in Mice

Sun Yan-Li,Wang Xue-Lin,Yang Lei-Lei,Ge Zhao-Jia,Zhao Yong,Luo Shi-Ming,Shen Wei,Sun Qing-Yuan,Yin Shen

Paraquat (PQ) is a widely used non-selective and oxidizing herbicide in farmland, orchards, flower nursery, and grassland. Overuse of PQ will accumulate in the body and affect the reproduction in mammals. In this study, we found that PQ could reduce the female fertility by oral administration for 21 days in mice. PQ exposure could impair the nuclear maturation by perturbing the spindle assembly and kinetochore–microtubule attachment to cause the misaligned chromosomes during meiosis. In the meantime, PQ exposure disturbed the mitochondrial distribution and enhanced the level of reactive oxygen species and early apoptosis, which thereby deteriorated the early embryo development. Also, PQ administration could cause some changes in epigenetic modifications such as the level of H3K9me2 and H3K27me3. Therefore, PQ administration reduces the female fertility by impairing the nuclear and cytoplasmic maturation of oocytes in mice.

研究领域: 生殖生物学 · 毒理学 · 分子生物学

✓ 已验证 DOI PubMed 高影响因子

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Discovery of novel steroidal pyran–oxindole hybrids as cytotoxic agents

Paraquat Reduces the Female Fertility by Impairing the Oocyte Maturation in Mice