Discovery of novel N-benzylarylamide-dithiocarbamate based derivatives as dual inhibitors of tubulin polymerization and LSD1 that inhibit gastric cancers

Discovery of natural product-like spirooxindole derivatives as highly potent and selective LSD1/KDM1A inhibitors for AML treatment

(2022) Chao Yang et al.   BIOORGANIC CHEMISTRY

A Phase Ib/II Study of Sabizabulin, a Novel Oral Cytoskeleton Disruptor, in Men with Metastatic Castration-resistant Prostate Cancer with Progression on an Androgen Receptor–targeting Agent

(2022) Mark C. Markowski et al.   CLINICAL CANCER RESEARCH

Discovery of novel sulphonamide hybrids that inhibit LSD1 against bladder cancer cells

(2022) Jia Liu et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Discovery of a Novel Stilbene Derivative as a Microtubule Targeting Agent Capable of Inducing Cell Ferroptosis

(2022) Jingwei Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

SAR of Novel 3-Arylisoquinolinones: meta-Substitution on the Aryl Ring Dramatically Enhances Antiproliferative Activity through Binding to Microtubules

(2022) Mai A. Elhemely et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors

(2022) Chunpu Li et al.   JOURNAL OF MEDICINAL CHEMISTRY

A novel aromatic amide derivative SY-65 co-targeted tubulin and histone deacetylase 1 with potent anticancer activity in vitro and in vivo

(2022) Yin-Ru Li et al.   BIOCHEMICAL PHARMACOLOGY

Discovery of 4-methoxy-N-(1-naphthyl)benzenesulfonamide derivatives as small molecule dual-target inhibitors of tubulin and signal transducer and activator of transcription 3 (STAT3) based on ABT-751

(2022) Xuebao Wang et al.   BIOORGANIC CHEMISTRY

Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities

(2022) Jian Song et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of (2-(pyrrolidin-1-yl)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone as a novel potent tubulin depolymerizing and vascular disrupting agent

(2022) Chao Tian et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site

(2022) Xiang-Yu Yan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models

(2022) Martina Menna et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a Novel Vascular Disrupting Agent Inhibiting Tubulin Polymerization and HDACs with Potent Antitumor Effects

(2022) Huajian Zhu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, biological evaluation and docking studies of methylene bearing cyanopyrimidine derivatives possessing a hydrazone moiety as potent Lysine specific demethylase-1 (LSD1) inhibitors: A promising anticancer agents

(2022) Sharba Tasneem et al.   BIOORGANIC CHEMISTRY

Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway

(2022) Jian Song et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and structure–activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects

(2022) Yasushi Hattori et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: Further chemical modifications and potential therapeutic effects against lymphomas

(2022) Marilia Barreca et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1

(2021) Xing-Jie Dai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer

(2021) Ying-Chao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities

(2021) Huajian Zhu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel Benzimidazole and Indazole Analogues as Tubulin Polymerization Inhibitors with Potent Anticancer Activities

(2021) Yichang Ren et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors

(2021) Xiangyu Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Efficient Synthesis and Bioevaluation of Novel Dual Tubulin/Histone Deacetylase 3 Inhibitors as Potential Anticancer Agents

(2021) Xiaopeng Peng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Recent Progress on Tubulin Inhibitors with Dual Targeting Capabilities for Cancer Therapy

(2021) Wen Shuai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR

(2021) Jun Yan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities

(2021) Ya-Xin Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Installation of Pargyline, a LSD1 Inhibitor, in the HDAC Inhibitory Template Culminated in the Identification of a Tractable Antiprostate Cancer Agent

(2021) Ritu Ojha et al.   JOURNAL OF MEDICINAL CHEMISTRY

Therapeutic potential of targeting LSD1/ KDM1A in cancers

(2021) Xiangyu Zhang et al.   PHARMACOLOGICAL RESEARCH

Analysis of Dual Class I Histone Deacetylase and Lysine Demethylase Inhibitor Domatinostat (4SC-202) on Growth and Cellular and Genomic Landscape of Atypical Teratoid/Rhabdoid

(2020) Mariah M. Hoffman et al.   Cancers

Synthesis, Biological Evaluation, and Molecular Docking of Arylpyridines as Antiproliferative Agent Targeting Tubulin

(2020) JiaPeng He et al.   ACS Medicinal Chemistry Letters

Synthesis and biological evaluation of benzofuran-based 3,4,5-trimethoxybenzamide derivatives as novel tubulin polymerization inhibitors

(2020) Qiu Li et al.   BIOORGANIC CHEMISTRY

Indolizine-phenothiazine hybrids as the first dual inhibitors of tubulin polymerization and farnesyltransferase with synergistic antitumor activity

(2020) Iuliana-Monica Moise et al.   BIOORGANIC CHEMISTRY

Phase I Study of Lysine-Specific Demethylase-1 Inhibitor CC-90011 in Patients With Advanced Solid Tumors and Relapsed/Refractory Non-Hodgkin Lymphoma

(2020) Antoine Hollebecque et al.   CLINICAL CANCER RESEARCH

First-in-Human Phase I Study of Iadademstat (ORY-1001): A First-in-Class Lysine-Specific Histone Demethylase 1A Inhibitor, in Relapsed or Refractory Acute Myeloid Leukemia

(2020) Olga Salamero et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1)

(2020) Toufike Kanouni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Orally available tubulin inhibitor VERU-111 enhances antitumor efficacy in paclitaxel-resistant lung cancer

(2020) Foyez Mahmud et al.   CANCER LETTERS

A novel orally active microtubule destabilizing agent S-40 targets the colchicine-binding site and shows potent antitumor activity

(2020) Tingting Du et al.   CANCER LETTERS

Discovery of orally active chalcones as histone lysine specific demethylase 1 inhibitors for the treatment of leukaemia

(2020) Yang Li et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2-d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors

(2019) Romeo Romagnoli et al.   JOURNAL OF MEDICINAL CHEMISTRY

LSD1/KDM1A inhibitors in clinical trials: advances and prospects

(2019) Yuan Fang et al.   Journal of Hematology & Oncology

1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase

(2018) Mei-Jung Lai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Identification of osimertinib (AZD9291) as a lysine specific demethylase 1 inhibitor

(2018) Zhong-Rui Li et al.   BIOORGANIC CHEMISTRY

Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

(2017) Thomas Bohnacker et al.   Nature Communications

Design, synthesis and molecular docking of novel diarylcyclohexenone and diarylindazole derivatives as tubulin polymerization inhibitors

(2016) Riham I. Ahmed et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors

(2016) Dong Cao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin

(2016) Pengfei Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Blocking Blood Flow to Solid Tumors by Destabilizing Tubulin: An Approach to Targeting Tumor Growth

(2016) María-Jesús Pérez-Pérez et al.   JOURNAL OF MEDICINAL CHEMISTRY

LSD1: biologic roles and therapeutic targeting

(2016) Alba Maiques-Diaz et al.   Epigenomics

A Phase I/II Trial of BNC105P with Everolimus in Metastatic Renal Cell Carcinoma

(2015) S. Pal et al.   CLINICAL CANCER RESEARCH

Design, Synthesis, and Structure–Activity Relationship of Novel LSD1 Inhibitors Based on Pyrimidine–Thiourea Hybrids As Potent, Orally Active Antitumor Agents

(2015) Li-Ying Ma et al.   JOURNAL OF MEDICINAL CHEMISTRY

Multi-target pharmacology: possibilities and limitations of the “skeleton key approach” from a medicinal chemist perspective

(2015) Alan Talevi   Frontiers in Pharmacology

Phase I Safety, Pharmacokinetic and Pharmacodynamic Evaluation of the Vascular Disrupting Agent Ombrabulin (AVE8062) in Patients with Advanced Solid Tumors

(2013) C. Sessa et al.   CLINICAL CANCER RESEARCH

Triazole–Dithiocarbamate Based Selective Lysine Specific Demethylase 1 (LSD1) Inactivators Inhibit Gastric Cancer Cell Growth, Invasion, and Migration

(2013) Yi-Chao Zheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

An Overview of Tubulin Inhibitors That Interact with the Colchicine Binding Site

(2012) Yan Lu et al.   PHARMACEUTICAL RESEARCH

Microtubule-binding agents: a dynamic field of cancer therapeutics

(2010) Charles Dumontet et al.   NATURE REVIEWS DRUG DISCOVERY

Microtubule inhibitors: Differentiating tubulin-inhibiting agents based on mechanisms of action, clinical activity, and resistance

(2009) E. A. Perez   MOLECULAR CANCER THERAPEUTICS