anti-cancer compounds

Oxindole (Indolin-2-one) 是一种芳族杂环砌块，其衍生物是激酶抑制剂研究中的主要成分。

1-Stearoyl-2-docosahexaenoyl-sn-glycero-3-phosphoethanolamine（18:0-22:6 PE）是一种用于构建脂质体的关键脂质成分。脂质体以其同心磷脂双层膜结构主要用于抗癌和抗感染的药物递送系统中。该化合物能够在其水性内部空间包裹高极性水溶性药物，同时将亲脂药物整合入脂质双层。它尤其适用于递送反义寡核苷酸，有效解决细胞内吸收不足和药物体内迅速丢失的问题。

Pixatimod（亦称PG-545）是一种合成糖类改良的肝素硫酸仿生物及Toll样受体9（TLR9）的激动剂，具有潜在的免疫增强、抗肿瘤和抗病毒作用。Pixatimod (PG545) 强效地通过破坏刺突蛋白-ACE2相互作用抑制SARS-CoV-2。此外，Pixatimod阻断多种促癌过程，包括细胞增殖、侵袭、转移、血管生成和上皮-间充质转化。这些作用在多种不同的小鼠癌症模型中展现出强大的效力，包括约30种异种移植模型和20种同种移植模型。Pixatimod已与多种批准的抗癌化合物联合测试，展示了其临床潜力，包括与gemcitabine、paclitaxel、sorafenib、铂类化合物及抗PD-1抗体合用。

Pixatimod（又名PG-545）是一种合成的改性糖类肝素硫酸模拟剂及Toll样受体9（TLR9）的激动剂，具有潜在的免疫刺激、抗肿瘤和抗病毒活性。Pixatimod强效抑制SARS-CoV-2，其通过破坏刺突蛋白-ACE2的相互作用来实现。此外，Pixatimod阻断了多种促癌过程，包括细胞增殖、侵袭、转移、血管生成及上皮-间充质转换。这些活性在多种不同的小鼠癌症模型中显示出强大效果，涵盖约30种异种移植模型和20种同源移植模型。Pixatimod已与多种已获批准的抗癌化合物联合测试，展现其临床潜力，包括与吉西他滨、紫杉醇、索拉非尼、铂类化合物和一种抗PD-1抗体的联合应用。

Sintilimab (IBI308) 是一种人源化的 IgG4 单克隆抗体，具有显著的抗肿瘤活性，通过与 PD-1 结合从而阻断 PD-1 与其配体 (PD-L1 和 PL-L2) 的相互作用，进而恢复内源性抗肿瘤 T 细胞反应。Sintilimab 联合其他化合物来治疗经典霍奇金淋巴瘤、非小细胞肺癌和食管癌。

Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition of both topoisomerases I and II, initiating DNA cleavage and apoptosis. Becatecarin, alone or in combination with other compounds, has anti-cancer as well as myelosuppressive effects in vivo. It is also a transport substrate of the ATP-binding cassette (ABC) transporter ABCG2.

NO-indomethacin is a hybrid molecule of indomethacin and a nitric oxide (NO) donor. This drug design combines the anti-inflammatory properties of a non-steroidal anti-inflammatory drug (NSAID) with the gastrointestinal protective effects of NO. Compounds of this class retain their anti-inflammatory and analgesic activity, but have reduced gastrointestinal and kidney toxicity compared to the NSAID alone. NO-indomethacin also enhances the cancer chemopreventative activity of indomethacin. NO-indomethacin exhibits an IC50 of 82 μM, compared to >1,000 μM for indomethacin alone, for the inhibition of pancreatic cancer cell (PaCa-2) growth after 24 hours in culture.

5'-O-DMT-ibu-rG is a valuable model for a novel category of DNA binding compounds, offering the potential for the creation of highly effective and specifically targeted anti-cancer medications.

Amrubicin, also known as SM-5887, is an anthracycline used in the treatment of lung cancer. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell growth inhibition and cell death. This agent has demonstrated a higher level of anti-tumor activity than conventional anthracycline drugs without exhibiting any indication of the cumulative cardiac toxicity common to this class of compounds. It is marketed in Japan since 2002 by Sumitomo Pharmaceuticals.

Mirvetuximab (M9346A) 是一种新型叶酸受体α (FRα) 靶向 anti-FOLR1 (folate receptor 1) 的单克隆抗体。Mirvetuximab soravtansine 常与铂类化合物或与其他化合物偶联成为抗体-药物偶联物用来治疗卵巢癌和其他 FRα 阳性的癌症。

SN38-PAB-Lys(MMT)-oxydiacetamide-PEG8-N3 是一款用于抗体药物偶联物 (ADC) 合成的化学试剂，由抗癌药物SN38与链接子Lys(MMT)-PAB-oxydiacetamide-PEG8-N3 构成，属于点击化学工具。该化合物含有Azide基团，它可通过铜催化的叠氮-炔点击反应 (CuAAc) 与含Alkyne基团的分子耦合，亦能通过应变促进的炔-叠氮点击反应 (SPAAC) 与含DBCO 或 BCN 基团的分子反应。