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• W2014671467 abstract "Targeting the SMAD3 protein is an attractive therapeutic strategy for treating cancer, as it avoids the potential toxicities due to targeting the TGF-β signaling pathway upstream. Compound SIS3 was the first selective SMAD3 inhibitor developed that had acceptable activity, but its poor water solubility limited its development. Here, a series of SIS3 analogs was created to investigate the structure–activity relationship for inhibiting the activation of SMAD3. On the basis of this SAR, further optimization generated a water-soluble compound, 16d, which was capable of effectively blocking SMAD3 activation in vitro and had similar NK cell-mediated anticancer effects in vivo to its parent SIS3. This study not only provided a preferable lead compound, 16d, for further drug discovery or a potential tool to study SMAD3 biology, but also proved the effectiveness of our strategy for water-solubility driven optimization." @default.
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• W2014671467 date "1993-01-01" @default.
• W2014671467 modified "2023-10-06" @default.
• W2014671467 title "Synthesis of lactams with potential cardiotonic activity" @default.
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• W2014671467 doi "https://doi.org/10.1016/0223-5234(93)90118-x" @default.
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