adenocarcinoma cell

3PO 是一种 PFKFB3 的小分子抑制剂，IC50值为22.9 μM。它抑制几种人类恶性造血和腺癌细胞系的增殖，IC50在1.4到24 μM 之间。它抑制葡萄糖摄取，并降低 Fru-2,6-BP、乳酸、ATP、NAD+ 和 NADH 的细胞内浓度。

Ellipticine (Elliptisine) 是一种有效的抗肿瘤剂，抑制 DNA 拓扑异构酶 II 活性，对白血病、神经母细胞瘤和胶质母细胞瘤有部分活性。

Vinaxanthone (SM-345431) 是一种从青霉菌中提取的小分子化合物，是一种具有选择性和有效性的 semaphorin3A、phospholipase C (PLC) 和 FabI 抑制剂，抑制semaphorin3A 和 FabI。Vinaxanthone 具有抗菌活性，阻止细胞内脂肪酸合成，抑制金黄色葡萄球菌的生长。

Bexlosteride (LY300502) 是一种苯并喹啉酮类人 I 型 5α-还原酶抑制剂。Bexlosteride 在 LNCaP 细胞培养物中显示出代谢抑制、抗增殖和抗分泌作用。Bexlosteride 可用于前列腺癌的研究。

LRH-1 Inhibitor-3是一种抑制LRH-1转录活性的拮抗剂，能够降低与细胞生长和增殖相关的靶基因表达，如SHP (small heterodimer partner)，cyclin E1 (CCNE1)和G0S2，抑制人类胰腺、结肠和乳腺腺癌细胞增殖。

PARP-1-IN-2 是一种有效且可透过血脑屏障的 PARP1 抑制剂（IC50： 149 nM）。PARP-1-IN-2 在细胞实验中对人肺腺癌上皮细胞系 A549 显示出显著的抗增殖活性。PARP-1-IN-2 可诱导 A549 细胞凋亡。

BPI-9016M is an effective, orally active, and selective dual inhibitor of c-Met and AXL tyrosine kinases. It suppresses tumor cell growth, invasion, and migration of lung adenocarcinoma.

SBI-797812 是在结构上类似于活性位点定向的 NAMPT 抑制剂的化合物，能够阻断这些抑制剂与 NAMPT 的结合。 它将 NAMPT 反应平衡转向 NMN 形成，提高 NAMPT 对 ATP 的亲和力，稳定 His247 处的磷酸化 NAMPT，增加焦磷酸盐副产物的消耗，并通过 NAD+钝化反馈抑制。

经化学修饰的四环素 （CMTs） 可抑制 MMPs，但缺乏抗菌活性。四环素的非抗菌衍生物称为 incyclinide (COL-3, CMT-3)。 实验证明，Incyclinide（CMT-3） 可抑制前列腺癌、结肠腺癌和黑色素瘤在细胞培养中的侵袭性，并抑制肿瘤的生长和转移。

PARP1-IN-31 (compound 11f) 为基于酞嗪酮的抗肺腺癌化合物，对PARP-1展示出抑制活性（IC50值为97 nM），能够在肺癌细胞系中诱导细胞凋亡和抑制细胞增殖。

UNBS3157是一种新型的非血液毒性萘酰亚胺衍生物，具有强大的抗肿瘤活性，能够通过DNA插入作用和毒化拓扑异构酶IIalpha来与DNA结合。与之相关的萘酰亚胺类化合物Amonafide在二期乳腺癌试验中表现出了活性，但由于限制剂量的骨髓毒性，目前尚未进入三期临床试验。相比之下，UNBS3157的最大耐受剂量比Amonafide高出3-4倍，并且在显示出显著抗肿瘤效果的剂量下未引起小鼠的血液毒性。此外，在活体内模型中，包括(i) L1210鼠白血病、(ii) MXT-HI鼠乳腺腺癌、以及(iii)人类A549非小细胞肺癌和BxPC3胰腺癌原位模型中，UNBS3157显示出优于Amonafide的效果。

SBI-183 是一种具有口服活性的 QSOX1 抑制剂 (Kd: 20 μM)，能够抑制肾癌细胞系、三阴性乳腺癌细胞系、肺腺癌细胞系和胰腺导管腺癌的增殖与侵袭表型。SBI-183 在体内可以抑制两种人肾细胞癌异种移植小鼠模型的肿瘤生长。

CHI-KAT8i5 是一种高选择性的KAT8抑制剂，具有 19.72 μM 的 KD。它能以剂量依赖性方式引发凋亡 (Apoptosis)，并抑制食管鳞状细胞癌、结肠癌、黑色素瘤、胃癌、非小细胞腺癌及肝癌的肿瘤生长。

Antiproliferative agent-66 (Compound B3) 是一种抗细胞增殖剂，能够诱导细胞凋亡 (apoptosis) 和促使细胞周期阻滞。其对 SH-SY5Y 神经母细胞瘤、HT-29 结直肠腺癌以及成纤维细胞的 IC50 为 2.03 至 3.6 µM。此外，Antiproliferative agent-66 作为微管蛋白聚合的抑制剂，其 IC50 为 0.79 µM。

DS-7423 是PI3K 和mTOR 的有效抑制剂，抑制PI3Kα 和 mTOR 的IC50分别为15.6 nM 和 34.9 nM。DS-7423表现出抗癌活性。

Aspulvinone O is a fungal metabolite that has been found in P. variotti and has antioxidant and anticancer activities.1,2 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals in a cell-free assay (IC50 = 11.6 μM).1 Aspulvinone O inhibits aspartate transaminase 1 (GOT1; Kd = 3.32 μM) and is cytotoxic to PANC-1, AsPC-1, and SW1990 pancreatic cancer cells (IC50s = 20.54-26.8 μM).2 It reduces the oxygen consumption rate (OCR) and induces apoptosis in SW1990 cells. Aspulvinone O (2.5 and 5 mg kg) reduces tumor growth in an SW1990 mouse xenograft model. |1. Zhang, P., Li, X.-M., Wang, J.-N., et al. New butenolide derivatives from the marine-derived fungus Paecilomyces variotii with DPPH radical scavenging activity. Phytochem. Lett. 11, 85-88 (2015).|2. Sun, W., Luan, S., Qi, C., et al. Aspulvinone O, a natural inhibitor of GOT1 suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism. Cell Commun. Signal. 17(1), 111 (2019).

Chromomycin A2 is an aureolic acid that has been found in several marine actinomycetes and has antibacterial and anticancer activities. Chromomycin A2 inhibits the growth of B. subtilis in an agar diffusion assay. It also inhibits the growth of human SGC7901 gastric cancer, HepG2 hepatocellular carcinoma, A549 lung epithelial adenocarcinoma, HCT116 colon cancer, and COC1 ovarian cancer cells, as well as human umbilical vein endothelial cells (HUVECs; IC50s = 4, 0.5, 3, 5, 5, and 8 nM, respectively). Chromomycin A2 (30 nM) halts the cell cycle in the G0 G1 phase and increases the protein levels of LC3A and LC3B in MALME-3M melanoma cells, indicating that it induces autophagy. It also increases the levels and promoter activity of the autophagic proteins ATG7 and ATG10 and reduces cell viability to 50% in human SCC-11 squamous cell carcinoma cells when used at a concentration of 30 nM.

Chrysomycin B 是分离自链霉菌的一种抗生素 。Chrysomycin B 能引起人肺腺癌 A549 细胞系的 DNA 损伤，并抑制拓扑异构酶 II。

Brevilin A 是从Centipeda minima 中分离的倍半萜内酯，具有抗癌活性。它通过线粒体途径和 PI3K AKT mTOR 失活诱导结肠腺癌细胞 CT26 的凋亡和自噬。它是一种选择性JAK-STAT 信号通路抑制剂，通过减弱 JAK 信号和 阻塞 STAT3 信号起作用。

Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by inducing disruption of mitochondrial homeostasis, cell cycle arrest, and apoptosis in human adenocarcinoma cells. Moreover, Antitumor agent-44 demonstrates significant anti-tumor activity in a lung cancer cell xenograft mice model [1].

Antitumor agent-75 是一种新型的、有效的抗肿瘤剂。Antitumor agent-75 对癌症和正常人类细胞系具有细胞毒性作用。Antitumor agent-75 结合使用 Antitumor agent-74 时对人肺腺癌（细胞系 A549 ）表现出高度选择性的细胞毒作用 (IC50: 2.8 μM)。Antitumor agent-75 能够用于研究癌症。

Deltarasin is a high affinity PDEδ-KRAS interaction inhibitor. Deltarasin can inhibit KRAS-PDEδ interactions by binding to a hydrophobic pocket on PDEδ, resulting in the impairment of cell growth, KRAS activity, and RAS RAF signaling in human pancreatic ductal adenocarcinoma cell lines. The anti-cancer cell activity of deltarasin can be enhanced by simultaneously blocking tumor protective autophagy

IST-622 is a unique topoisomerase inhibitor, showing significant growth-inhibitory effects against large-cell lung cancer (Lu-116) and gastric adenocarcinoma (St-4).

Oxythiamine chloride HCl is a thiamine antimetabolite that has anticancer activities. It is converted by thiamine pyrophosphokinase to oxythiamine pyrophosphate, a transketolase inhibitor. Oxythiamine decreases transketolase activity in breast cancer. It inhibits the nonoxidative synthesis of ribose and decreases RNA and DNA synthesis in pancreatic cancer. In vivo, oxythiamine induces cell cycle arrest at the G1 phase and apoptosis in an adenocarcinoma model. Oxythiamine, in combination with sorafenib, reduces tumor growth in an SMMC mouse xenograft model and has also been used to induce thiamine deficiency in mice.