FDA-Approved Small Molecule Compounds as Drugs for Solid Cancers from Early 2011 to the End of 2021

PROTAC targeted protein degraders: the past is prologue

(2022) Miklós Békés et al.   NATURE REVIEWS DRUG DISCOVERY

Global cancer statistics 2020: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2021) Hyuna Sung et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Pharmacokinetics of UGN-101, a mitomycin-containing reverse thermal gel instilled via retrograde catheter for the treatment of low-grade upper tract urothelial carcinoma

(2021) Ahmad Shabsigh et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer

(2021) Francois Gonzalvez et al.   Cancer Discovery

Targeting the Fibroblast Growth Factor Receptor (FGFR) Family in Lung Cancer

(2021) Laura Pacini et al.   Cells

The KRAS-G12C inhibitor: activity and resistance

(2021) Jiao Liu et al.   CANCER GENE THERAPY

Sotorasib: First Approval

(2021) Hannah A. Blair   DRUGS

Infigratinib: First Approval

(2021) Connie Kang   DRUGS

Thermo-responsive hydrogels for cancer local therapy: Challenges and state-of-art

(2021) Diana Rafael et al.   INTERNATIONAL JOURNAL OF PHARMACEUTICS

The current knowledge concerning solid cancer and therapy

(2021) Masoud Najafi et al.   JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer

(2021) Jun Liang et al.   JOURNAL OF MEDICINAL CHEMISTRY

RET Inhibitors in Non-Small-Cell Lung Cancer

(2021) Priscilla Cascetta et al.   Cancers

Role of Small Molecule Targeted Compounds in Cancer: Progress, Opportunities, and Challenges

(2021) Guoqiang Sun et al.   Frontiers in Cell and Developmental Biology

Mobocertinib: First Approval

(2021) Anthony Markham   DRUGS

Targeting mutated GTPase KRAS in tumor therapies

(2021) Guangjin Fan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

On target: Rational approaches to KRAS inhibition for treatment of non-small cell lung carcinoma

(2021) Colin R. Lindsay et al.   LUNG CANCER

FDA-Approved Drugs for Hematological Malignancies—The Last Decade Review

(2021) Aleksandra Sochacka-Ćwikła et al.   Cancers

Infigratinib (BGJ398) in previously treated patients with advanced or metastatic cholangiocarcinoma with FGFR2 fusions or rearrangements: mature results from a multicentre, open-label, single-arm, phase 2 study

(2021) Milind Javle et al.   Lancet Gastroenterology & Hepatology

Avapritinib: First Approval

(2020) Sohita Dhillon   DRUGS

An evaluation of glasdegib for the treatment of acute myelogenous leukemia

(2020) Xavier Thomas et al.   EXPERT OPINION ON PHARMACOTHERAPY

Sonidegib and vismodegib in the treatment of patients with locally advanced basal cell carcinoma: a joint expert opinion

(2020) R. Dummer et al.   JOURNAL OF THE EUROPEAN ACADEMY OF DERMATOLOGY AND VENEREOLOGY

Tepotinib: First Approval

(2020) Anthony Markham   DRUGS

Tazemetostat: First Approval

(2020) Sheridan M. Hoy   DRUGS

Pemigatinib: First Approval

(2020) Sheridan M. Hoy   DRUGS

Pemigatinib for previously treated, locally advanced or metastatic cholangiocarcinoma: a multicentre, open-label, phase 2 study

(2020) Ghassan K Abou-Alfa et al.   LANCET ONCOLOGY

Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models

(2020) Anita Kulukian et al.   MOLECULAR CANCER THERAPEUTICS

Selumetinib in Children with Inoperable Plexiform Neurofibromas

(2020) Andrea M. Gross et al.   NEW ENGLAND JOURNAL OF MEDICINE

Oral Relugolix for Androgen-Deprivation Therapy in Advanced Prostate Cancer

(2020) Neal D. Shore et al.   NEW ENGLAND JOURNAL OF MEDICINE

Tepotinib in Non–Small-Cell Lung Cancer with MET Exon 14 Skipping Mutations

(2020) Paul K. Paik et al.   NEW ENGLAND JOURNAL OF MEDICINE

Poly (ADP-Ribose) Polymerase Inhibitors: Talazoparib in Ovarian Cancer and Beyond

(2020) Stergios Boussios et al.   Drugs in research & development

Tyrosine Kinase Inhibitors in Cancer: Breakthrough and Challenges of Targeted Therapy

(2020) Charles Pottier et al.   Cancers

A Phase 2 Study of Abemaciclib in Patients with Brain Metastases Secondary to Hormone Receptor Positive Breast Cancer

(2020) Sara M Tolaney et al.   CLINICAL CANCER RESEARCH

Tucatinib: First Approval

(2020) Arnold Lee   DRUGS

Selumetinib: First Approval

(2020) Anthony Markham et al.   DRUGS

Selpercatinib: First Approval

(2020) Anthony Markham   DRUGS

Capmatinib: First Approval

(2020) Sohita Dhillon   DRUGS

Ripretinib: First Approval

(2020) Sohita Dhillon   DRUGS

Neratinib Plus Capecitabine Versus Lapatinib Plus Capecitabine in HER2-Positive Metastatic Breast Cancer Previously Treated With ≥ 2 HER2-Directed Regimens: Phase III NALA Trial

(2020) Cristina Saura et al.   JOURNAL OF CLINICAL ONCOLOGY

Amide Bond Bioisosteres: Strategies, Synthesis, and Successes

(2020) Shikha Kumari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Ripretinib in patients with advanced gastrointestinal stromal tumours (INVICTUS): a double-blind, randomised, placebo-controlled, phase 3 trial

(2020) Jean-Yves Blay et al.   LANCET ONCOLOGY

Radiopharmaceutical therapy in cancer: clinical advances and challenges

(2020) George Sgouros et al.   NATURE REVIEWS DRUG DISCOVERY

Lurbinectedin: First Approval

(2020) Anthony Markham   DRUGS

Efficacy of Selpercatinib in RET-Altered Thyroid Cancers

(2020) Lori J. Wirth et al.   NEW ENGLAND JOURNAL OF MEDICINE

Pembrolizumab in Combination with Axitinib as First-Line Treatment for Patients with Renal Cell Carcinoma (RCC): Evidence to Date

(2020) Vincent Chau et al.   Cancer Management and Research

PARP Inhibitors in Metastatic Prostate Cancer: Evidence to Date

(2020) Emily Nizialek et al.   Cancer Management and Research

Safety and Tolerability of c-MET Inhibitors in Cancer

(2019) Alberto Puccini et al.   DRUG SAFETY

Larotrectinib: First Global Approval

(2019) Lesley J. Scott   DRUGS

Lorlatinib: First Global Approval

(2019) Yahiya Y. Syed   DRUGS

Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants

(2019) Bryan D. Smith et al.   CANCER CELL

Relugolix: First Global Approval

(2019) Anthony Markham   DRUGS

Clinical development of targeted and immune based anti-cancer therapies

(2019) N. A. Seebacher et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Alpelisib for PIK3CA-Mutated, Hormone Receptor–Positive Advanced Breast Cancer

(2019) Fabrice André et al.   NEW ENGLAND JOURNAL OF MEDICINE

Alpelisib: First Global Approval

(2019) Anthony Markham   DRUGS

Erdafitinib: First Global Approval

(2019) Anthony Markham   DRUGS

Entrectinib: First Global Approval

(2019) Zaina T. Al-Salama et al.   DRUGS

Maintenance Olaparib for Germline BRCA-Mutated Metastatic Pancreatic Cancer

(2019) Talia Golan et al.   NEW ENGLAND JOURNAL OF MEDICINE

Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma

(2019) Yohann Loriot et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeted Radionuclide Therapy for Patients with Metastatic Pheochromocytoma and Paraganglioma: From Low-Specific-Activity to High-Specific-Activity Iodine-131 Metaiodobenzylguanidine

(2019) Camilo Jimenez et al.   Cancers

Targeted Therapy for Advanced Thyroid Cancer: Kinase Inhibitors and Beyond

(2019) Maria E Cabanillas et al.   ENDOCRINE REVIEWS

Capmatinib for the treatment of non-small cell lung cancer

(2019) Johan Filip Vansteenkiste et al.   Expert Review of Anticancer Therapy

Encorafenib, Binimetinib, and Cetuximab in BRAF V600E–Mutated Colorectal Cancer

(2019) Scott Kopetz et al.   NEW ENGLAND JOURNAL OF MEDICINE

Second-generation EGFR and ErbB tyrosine kinase inhibitors as first-line treatments for non-small cell lung cancer

(2019) Shouzheng Wang et al.   OncoTargets and Therapy

Lurbinectedin synergizes with immune checkpoint blockade to generate anticancer immunity

(2019) Wei Xie et al.   OncoImmunology

Second-Generation Antiandrogens: From Discovery to Standard of Care in Castration Resistant Prostate Cancer

(2019) Meghan A. Rice et al.   Frontiers in Oncology

Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015–2019)

(2019) Concepción Sánchez-Martínez et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Darolutamide: First Approval

(2019) Anthony Markham et al.   DRUGS

Pexidartinib: First Approval

(2019) Yvette N. Lamb   DRUGS

Small molecule combats cancer-causing KRAS protein at last

(2019) Roy S. Herbst et al.   NATURE

Overall Survival with Osimertinib in Untreated, EGFR-Mutated Advanced NSCLC

(2019) Suresh S. Ramalingam et al.   NEW ENGLAND JOURNAL OF MEDICINE

Irinotecan: 25 years of cancer treatment

(2019) Christian Bailly   PHARMACOLOGICAL RESEARCH

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry

(2019) Arun K. Ghosh et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tivozanib versus sorafenib in patients with advanced renal cell carcinoma (TIVO-3): a phase 3, multicentre, randomised, controlled, open-label study

(2019) Brian I Rini et al.   LANCET ONCOLOGY

Tucatinib, Trastuzumab, and Capecitabine for HER2-Positive Metastatic Breast Cancer

(2019) Rashmi K. Murthy et al.   NEW ENGLAND JOURNAL OF MEDICINE

Apalutamide: First Global Approval

(2018) Zaina T. Al-Salama   DRUGS

Alectinib: A Review in Advanced, ALK-Positive NSCLC

(2018) Julia Paik et al.   DRUGS

The safety of trifluridine and tipiracil for the treatment of metastatic colorectal cancer

(2018) Julia Martinez-Perez et al.   Expert Opinion On Drug Safety

Phosphatidylinositol 3-Kinase α–Selective Inhibition With Alpelisib (BYL719) in PIK3CA-Altered Solid Tumors: Results From the First-in-Human Study

(2018) Dejan Juric et al.   JOURNAL OF CLINICAL ONCOLOGY

Dabrafenib and Trametinib Treatment in Patients With Locally Advanced or Metastatic BRAF V600–Mutant Anaplastic Thyroid Cancer

(2018) Vivek Subbiah et al.   JOURNAL OF CLINICAL ONCOLOGY

Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study

(2018) Antoine Italiano et al.   LANCET ONCOLOGY

Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF -mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial

(2018) Reinhard Dummer et al.   LANCET ONCOLOGY

Preliminary results for avelumab plus axitinib as first-line therapy in patients with advanced clear-cell renal-cell carcinoma (JAVELIN Renal 100): an open-label, dose-finding and dose-expansion, phase 1b trial

(2018) Toni K Choueiri et al.   LANCET ONCOLOGY

Encorafenib and Binimetinib: First Global Approvals

(2018) Matt Shirley   DRUGS

Targeting oncogenic Raf protein-serine/threonine kinases in human cancers

(2018) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Dacomitinib: First Global Approval

(2018) Matt Shirley   DRUGS

Talazoparib: First Global Approval

(2018) Sheridan M. Hoy   DRUGS

Larotrectinib for the treatment of TRK fusion solid tumors

(2018) Theodore W. Laetsch et al.   Expert Review of Anticancer Therapy

Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs

(2018) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Encorafenib/binimetinib for the treatment of BRAF-mutant advanced, unresectable, or metastatic melanoma: design, development, and potential place in therapy

(2018) James Sun et al.   OncoTargets and Therapy

CDK 4/6 Inhibitors as Single Agent in Advanced Solid Tumors

(2018) Francesco Schettini et al.   Frontiers in Oncology

Cabozantinib for the treatment of kidney cancer

(2017) Ahmed Abdelaziz et al.   Expert Review of Anticancer Therapy

Targeted radionuclide therapy in combined-modality regimens

(2017) Martin R Gill et al.   LANCET ONCOLOGY

Looking Back, Looking Forward at Halogen Bonding in Drug Discovery

(2017) Lois Mendez et al.   MOLECULES

Sonidegib: mechanism of action, pharmacology, and clinical utility for advanced basal cell carcinomas

(2017) Sachin Jain et al.   OncoTargets and Therapy

Safety and Antitumor Activity of the Multitargeted Pan-TRK, ROS1, and ALK Inhibitor Entrectinib: Combined Results from Two Phase I Trials (ALKA-372-001 and STARTRK-1)

(2017) Alexander Drilon et al.   Cancer Discovery

Axitinib in the treatment of renal cell carcinoma: design, development, and place in therapy

(2017) Audrey Bellesoeur et al.   Drug Design Development and Therapy

Radium 223 dichloride for prostate cancer treatment

(2017) Emmanuel Deshayes et al.   Drug Design Development and Therapy

A phase II trial of abiraterone acetate plus prednisone in patients with triple-negative androgen receptor positive locally advanced or metastatic breast cancer (UCBG 12-1)

(2016) H. Bonnefoi et al.   ANNALS OF ONCOLOGY

Minor modifications to ceritinib enhance anti-tumor activity in EML4-ALK positive cancer

(2016) Chung Hyo Kang et al.   CANCER LETTERS

Lenvatinib: Role in thyroid cancer and other solid tumors

(2016) Maria E. Cabanillas et al.   CANCER TREATMENT REVIEWS

U.S. Food and Drug Administration Approval: Cabozantinib for the Treatment of Advanced Renal Cell Carcinoma

(2016) Harpreet Singh et al.   CLINICAL CANCER RESEARCH

FDA Approval of Palbociclib in Combination with Fulvestrant for the Treatment of Hormone Receptor-Positive, HER2-Negative Metastatic Breast Cancer

(2016) A. J. Walker et al.   CLINICAL CANCER RESEARCH

Osimertinib: First Global Approval

(2016) Sarah L. Greig   DRUGS

Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase

(2016) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nanoliposomal irinotecan with fluorouracil and folinic acid in metastatic pancreatic cancer after previous gemcitabine-based therapy (NAPOLI-1): a global, randomised, open-label, phase 3 trial

(2016) Andrea Wang-Gillam et al.   LANCET

Lurbinectedin Specifically Triggers the Degradation of Phosphorylated RNA Polymerase II and the Formation of DNA Breaks in Cancer Cells

(2016) G. Santamaria Nunez et al.   MOLECULAR CANCER THERAPEUTICS

Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications

(2016) E. Ardini et al.   MOLECULAR CANCER THERAPEUTICS

Onivyde for the therapy of multiple solid tumors

(2016) Haijun Zhang   OncoTargets and Therapy

Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-Small Cell Lung Cancer, and Other Solid Tumors

(2016) A. Patnaik et al.   Cancer Discovery

FDA Approval: Palbociclib for the Treatment of Postmenopausal Patients with Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer

(2015) J. A. Beaver et al.   CLINICAL CANCER RESEARCH

Palbociclib: First Global Approval

(2015) Sohita Dhillon   DRUGS

Sonidegib: First Global Approval

(2015) Celeste B. Burness   DRUGS

Cobimetinib: First Global Approval

(2015) Karly P. Garnock-Jones   DRUGS

Lenvatinib: First Global Approval

(2015) Lesley J. Scott   DRUGS

Olaparib: First Global Approval

(2015) Emma D. Deeks   DRUGS

Olaparib: an oral PARP-1 and PARP-2 inhibitor with promising activity in ovarian cancer

(2015) Camille C Gunderson et al.   Future Oncology

Akt inhibitors in cancer treatment: The long journey from drug discovery to clinical use (Review)

(2015) GEORGE MIHAI NITULESCU et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor

(2015) William D. Tap et al.   NEW ENGLAND JOURNAL OF MEDICINE

Irinotecan, a key chemotherapeutic drug for metastatic colorectal cancer

(2015) Ken-ichi Fujita   WORLD JOURNAL OF GASTROENTEROLOGY

Tivozanib: Status of Development

(2015) Muhammad Omer Jamil et al.   Current Oncology Reports

Mechanisms of resistance to EGFR tyrosine kinase inhibitors

(2015) Lihua Huang et al.   Acta Pharmaceutica Sinica B

A Novel Multiple Tyrosine-kinase Targeted Agent to Explore the Future Perspectives of Anti-Angiogenic Therapy for the Treatment of Multiple Solid Tumors: Cabozantinib

(2014) Subhajit Roy et al.   Anti-Cancer Agents in Medicinal Chemistry

Ceritinib: First Global Approval

(2014) Sohita Dhillon et al.   DRUGS

Radium-223 Dichloride: A Review of Its Use in Patients with Castration-Resistant Prostate Cancer with Symptomatic Bone Metastases

(2014) Matt Shirley et al.   DRUGS

ARRY-334543 Reverses Multidrug Resistance by Antagonizing the Activity of ATP-Binding Cassette Subfamily G Member 2

(2014) De-Shen Wang et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs

(2014) Chong Wang et al.   Nature Communications

The ALK Inhibitor Ceritinib Overcomes Crizotinib Resistance in Non-Small Cell Lung Cancer

(2014) L. Friboulet et al.   Cancer Discovery

Role of Macrophage Targeting in the Antitumor Activity of Trabectedin

(2013) Giovanni Germano et al.   CANCER CELL

Abiraterone Acetate in Combination with Prednisone for the Treatment of Patients with Metastatic Castration-Resistant Prostate Cancer: U.S. Food and Drug Administration Drug Approval Summary

(2013) P. G. Kluetz et al.   CLINICAL CANCER RESEARCH

U.S. Food and Drug Administration Approval: Vismodegib for Recurrent, Locally Advanced, or Metastatic Basal Cell Carcinoma

(2013) M. Axelson et al.   CLINICAL CANCER RESEARCH

Enzalutamide for Treatment of Patients with Metastatic Castration-Resistant Prostate Cancer Who Have Previously Received Docetaxel: U.S. Food and Drug Administration Drug Approval Summary

(2013) Y. M. Ning et al.   CLINICAL CANCER RESEARCH

Radium Ra 223 Dichloride Injection: U.S. Food and Drug Administration Drug Approval Summary

(2013) P. G. Kluetz et al.   CLINICAL CANCER RESEARCH

Review of Poly (ADP-ribose) Polymerase (PARP) Mechanisms of Action and Rationale for Targeting in Cancer and Other Diseases

(2013) Julio Morales et al.   CRITICAL REVIEWS IN EUKARYOTIC GENE EXPRESSION

Trametinib: First Global Approval

(2013) Cameron J. M. Wright et al.   DRUGS

Dabrafenib: First Global Approval

(2013) Anita D. Ballantyne et al.   DRUGS

Afatinib: First Global Approval

(2013) Rosselle T. Dungo et al.   DRUGS

Data-Mining for Sulfur and Fluorine: An Evaluation of Pharmaceuticals To Reveal Opportunities for Drug Design and Discovery

(2013) Elizabeth A. Ilardi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Vascularity of primary and metastatic renal cell carcinoma specimens

(2013) Saadia A Aziz et al.   Journal of Translational Medicine

Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors

(2012) J. Murai et al.   CANCER RESEARCH

Vandetanib

(2012) James E. Frampton   DRUGS

Regorafenib for cancer

(2012) Dirk Strumberg et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Abiraterone acetatefor the treatment of prostate cancer

(2012) Charles J Ryan et al.   EXPERT OPINION ON PHARMACOTHERAPY

Dabrafenib and its potential for the treatment of metastatic melanoma

(2012) Rajmohan Murali et al.   Drug Design Development and Therapy

Vemurafenib

(2011) Keith. T Flaherty et al.   NATURE REVIEWS DRUG DISCOVERY

Crizotinib

(2011) Alice T. Shaw et al.   NATURE REVIEWS DRUG DISCOVERY

PM01183, a new DNA minor groove covalent binder with potent in vitro and in vivo anti-tumour activity

(2010) JFM Leal et al.   BRITISH JOURNAL OF PHARMACOLOGY

Nitrile-Containing Pharmaceuticals: Efficacious Roles of the Nitrile Pharmacophore

(2010) Fraser F. Fleming et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Review of Trabectedin (ET-743): A Unique Mechanism of Action

(2010) Maurizio D'Incalci et al.   MOLECULAR CANCER THERAPEUTICS

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

Mechanisms of Hedgehog pathway activation in cancer and implications for therapy

(2009) Suzie J. Scales et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Phosphatidylinositol 3-kinase inhibitors: promising drug candidates for cancer therapy

(2008) Dexin Kong et al.   CANCER SCIENCE

Axitinib for renal cell carcinoma

(2008) Guru Sonpavde et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

Recent Advances in the Development of Multi-Kinase Inhibitors

(2008) Martin Krug et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY